A new isoprenyl-phenol-type meroterpenoid from mangrove endophytic fungus sp. GXNU-Y65.

Asperphenol A (), a new isoprenyl-phenol-type meroterpenoid, was isolated from the mangrove endophytic fungus sp. GXNU-Y65 together with five known compounds (-. All structures were assigned using extensive NMR spectroscopic data and electronic circular dichroism (ECD) calculations.

A new isopimarane-type diterpene with anti-inflammatory activity from the .

A new isopimarane-type diterpene clinacanoid A () together with seven known terpenoids () were obtained from the . Their structures were elucidated based on extensive spectroscopic analysis (NMR, HR-ESI-MS), and the absolute configuration of was established based on single crystal X-ray diffraction. The inhibitory activity of all the compounds on NO production in lipopolysaccharide-induced (LPS) mouse leukemic monocyte macrophage RAW264.

Synthesis and anticancer mechanisms of four novel platinum(II) 4'-substituted-2,2':6',2''-terpyridine complexes.

Mitophagy, a selective autophagic process, has emerged as a pathway involved in degrading dysfunctional mitochondria. Herein, new platinum(II)-based chemotherapeutics with mitophagy-targeting properties are proposed. Four novel binuclear anticancer Pt(II) complexes with 4'-substituted-2,2':6',2''-terpyridine derivatives (tpy1-tpy4), , [Pt(tpy1)(DMSO)Cl]·CHOH (tpy1Pt), [Pt(tpy2)Cl][Pt(DMSO)Cl]·CHCOCH (tpy2Pt), [Pt(tpy3)Cl][Pt(DMSO)Cl] (tpy3Pt), and [Pt(tpy4)Cl]Cl·CHOH (tpy4Pt), were designed and prepared.

Synthesis and anticancer mechanisms of zinc(II)-8-hydroxyquinoline complexes with 1,10-phenanthroline ancillary ligands.

Twenty new zinc(II) complexes with 8-hydroxyquinoline (H-Q1-H-Q6) in the presence of 1,10-phenanthroline derivatives (D1-D10) were synthesized and formulated as [Zn(Q1)(D1)] (DQ1), [Zn(Q2)(D2)]·CHOH (DQ2), [Zn(Q1)(D3)] (DQ3), [Zn(Q1)(D4)] (DQ4), [Zn(Q3)(D5)] (DQ5), [Zn(Q3)(D4)] (DQ6), [Zn(Q4)(D5)]·CHOH (DQ7), [Zn(Q4)(D6)] (DQ8), [Zn(Q4)(D3)]·CHOH (DQ9), [Zn(Q4)(D1)]·HO (DQ10), [Zn(Q5)(D4)] (DQ11), [Zn(Q6)(D6)]·CHOH (DQ12), [Zn(Q5)(D2)]·5CHOH·HO (DQ13), [Zn(Q5)(D7)]·CHOH (DQ14), [Zn(Q5)(D8)]·CHCl (DQ15), [Zn(Q5)(D9)] (DQ16), [Zn(Q5)(D1)] (DQ17), [Zn(Q5)(D5)] (DQ18), [Zn(Q5)(D10)]·CHCl (DQ19) and [Zn(Q5)(D3)] (DQ20). They were characterized using multiple techniques. The cytotoxicity of DQ1-DQ20 was screened using human cisplatin-resistant SK-OV-3/DDP ovarian cancer (SK-OV-3CR) cells and normal hepatocyte (HL-7702) cells.

Novel bifluorescent Zn(II)-cryptolepine-cyclen complexes trigger apoptosis induced by nuclear and mitochondrial DNA damage in cisplatin-resistant lung tumor cells.

Four novel bifluorescent Zn(II)-cryptolepine-cyclen complexes, namely [Zn(BQTC)]Cl (Zn(BQTC)), [Zn(BQA) (Cur)Cl] (Zn(BQACur)), [Zn (TC)]Cl (Zn(TC)), and [Zn (AP) (Cur)Cl] (Zn(APCur)), bearing curcumin (H-Cur), cyclen (TC), 1,10-phenanthrolin-5-amine (AP), and novel cryptolepine-cyclen derivatives (BQTC and BQA) were prepared for cell nucleus- and mitochondria-specific imaging. MTT assay results indicated that Zn(BQTC) and Zn(BQACur) exhibit stronger anticancer activity against cisplatin-resistant A549R lung tumor cells than ZnCl, Zn(TC), Zn(APCur), H-Cur, TC, AP, BQTC, and BQA. Due to the dual fluorescence characteristic of Zn(BQTC), selective fluorescence imaging of the nucleus and mitochondria of A549R cancer cells was conducted.

Complexes of Zn(II) with a mixed tryptanthrin derivative and curcumin chelating ligands as new promising anticancer agents.

In this study, two novel curcumin (H-Cur)-tryptanthrin metal compounds-[Zn(TA)Cl], , Zn(TA), and [Zn(TA)(Cur)]Cl, , Zn(TAC)-were synthesized and investigated using 5-(bis-pyridin-2-ylmethyl-amino)-pentanoic acid (6,12-dioxo-6,12-dihydro-indolo[2,1-]quinazolin-8-yl)-amide (TA) and H-Cur as the targeting and high-activity anticancer chemotherapeutic moieties, respectively. They were then compared with the di-(2-picolyl)amine (PA) Zn(II) complex [Zn(PA)Cl], , Zn(PA). When compared with Zn(PA) and cisplatin, the IC values of Zn(TA) and Zn(TAC) indicated that the compounds had high cytotoxicity against A549/DDP cancer cells, implying that the H-Cur-tryptanthrin Zn(II) compounds have the potential for use as anticancer drugs.

Mitochondria-localizing curcumin-cryptolepine Zn(II) complexes and their antitumor activity.

Many metal complexes are potent candidates as mitochondrial-targeting agents. In this study, four novel Zn(II) complexes, [Zn(BPQA)Cl] (Zn1), [Zn(BPQA)(Curc)]Cl (Zn2), [Zn(PQA)Cl] (Zn3), and [Zn(PQA)(Curc)]Cl (Zn4), containing N,N-bis(pyridin-2-ylmethyl)benzofuro[3,2-b]quinolin-11-amine (BPQA), N-(pyridin-2-ylmethyl)benzofuro[3,2-b]quinolin-11-amine (PQA), and curcumin (H-Curc) were synthesized. An MTT assay showed that Zn1-Zn4 had strong anticancer activities against SK-OV-3/DDP and T-24 tumor cells with IC values of 0.

Imaging and therapeutic applications of Zn(ii)-cryptolepine-curcumin molecular probes in cell apoptosis detection and photodynamic therapy.

Novel red Zn(ii) complex-based fluorescent probes featuring cryptolepine-curcumin derivatives, namely, [Zn(BQ)Cl] (BQ-Zn) and [Zn(BQ)(Cur)]Cl (BQCur-Zn), were developed for the simple and fluorescent label-free detection of apoptosis, an important biological process. The probes could synergistically promote mitochondrion-mediated apoptosis and enhance tumor therapeutic effects in vitro and vivo.

Complexes of oxoplatin with rhein and ferulic acid ligands as platinum(iv) prodrugs with high anti-tumor activity.

We herein designed two new Pt prodrugs of oxoplatin (cis,cis,cis-[PtCl(NH)(OH)]), [PtCl(NH)(OC-FA)] (Pt-2) and [PtCl(NH)(OC-RH)] (Pt-3), by conjugating with ferulic acid (FA-COOH) and rhein (RH-COOH) which have well-known biological activities. Three other Pt(iv) complexes of [PtCl(NH)(OC-BA)] (Pt-1), [PtCl(NH)(OC-CA)] (Pt-4) and [PtCl(NH)(OC-TCA)] (Pt-5) (where BA-COOH = benzoic acid, CA-COOH = crotonic acid and TCA-COOH = trans-cinnamic acid) were also prepared for the comparative study. Like most Pt prodrug complexes, the cytotoxicity of Pt-3 containing the biologically active rhein (RH-COOH) ligand against lung carcinoma (A549 and A549/DDP) cells was higher than those of Pt-1, Pt-2, Pt-4, cisplatin and Pt-5.

Strong in vitro and vivo cytotoxicity of novel organoplatinum(II) complexes with quinoline-coumarin derivatives.

A series of novel organoplatinum(II) complexes, [Pt(QC1)(H-QC1)Cl] (Pt1), [Pt(QC2)(H-QC2)Cl] (Pt2), [Pt(QC3)(H-QC3)Cl] (Pt3), [Pt(QC4)(H-QC4)Cl]⋅CHOH (Pt4), [Pt(QC5)(H-QC5)Cl] (Pt5), [Pt(H-QC6)(DMSO)Cl] (Pt6), [Pt(H-QC7)(DMSO)Cl]⋅HO (Pt7), [Pt(H-QC8)(DMSO)Cl] (Pt8), [Pt(H-QC9)(DMSO)Cl]⋅CHOH (Pt9), [Pt(H-QC10)(DMSO)Cl] (Pt10) and [Pt(H-QC11)(DMSO)Cl] (Pt11), bearing quinoline-coumarin derivatives (H-QC1-H-QC11) have been first designed. Complexes Pt1-Pt11 selectively displayed obvious cytotoxicities in comparison to cisplatin for A549/DDP (cisplatin-resistant human lung adenocarcinoma) cells and HeLa cervical carcinoma cells, with IC values as low as 100 nM-10.33 μM.

Two telomerase-targeting Pt(ii) complexes of jatrorrhizine and berberine derivatives induce apoptosis in human bladder tumor cells.

Two novel Pt(ii) complexes, [Pt(B-TFA)Cl]Cl (Pt1) and [Pt(J-TFA)Cl]Cl (Pt2) with jatrorrhizine and berberine derivatives (B-TFA and J-TFA) were first prepared as desirable luminescent agents for cellular applications and potent telomerase inhibitors, which can induce bladder T-24 tumor cell apoptosis by targeting telomerase, together with induction of mitochondrial dysfunction, telomere DNA damage and cell-cycle arrest. Importantly, T-24 tumor inhibition rate (TIR) was 50.4% for Pt2, which was higher than that of Pt1 (26.

High in vitro and in vivo antitumor activities of luminecent platinum(II) complexes with jatrorrhizine derivatives.

Two highly active anticancer Pt(II) complexes, [Pt(Jat1)Cl]Cl (Pt1) and [Pt(Jat2)Cl]Cl (Pt2), containing jatrorrhizine derivative ligands (Jat1 and Jat2) are described. Cell intake study showed high accumulation in cell nuclear fraction. Pt1 and Pt2 exhibited high selectivity for HeLa cancer cells (IC = 15.

High in Vitro and in Vivo Tumor-Selective Novel Ruthenium(II) Complexes with 3-(2'-Benzimidazolyl)-7-fluoro-coumarin.

Three novel Ru(II) complexes, namely, (RuCl[L][DMSO])·HO (), (RuCl[L][DMSO]) (), and (RuCl[L][DMSO]) (), which respectively contain 3-(2'-benzimidazolyl)coumarin (L), 3-(2'-benzimidazolyl)-7-fluoro-coumarin (L), and 3-(2'-benzimidazolyl)-7-methoxyl-coumarin (L), were first designed and characterized. showed potent antitumor activity against NCI-H460 cells (IC = 0.30 ± 0.

Complexes of lanthanides(iii) with mixed 2,2'-bipyridyl and 5,7-dibromo-8-quinolinoline chelating ligands as a new class of promising anti-cancer agents.

Five novel lanthanides(iii) complexes, [Lu(Me)(MBrQ)2NO3] (MeMBrQ-Lu), [Ho(MeO)(MBrQ)2NO3] (MeOMBrQ-Ho), [Ho(Me)(MBrQ)2NO3] (MeMBrQ-Ho), [La(Me)2(BrQ)2NO3] (MeBrQ-La) and [Sm(Me)(BrQ)2(CH3OH)NO3] (MeBrQ-Sm), have been synthesized, in which 2,2'-bipyridyl (4,4'-dimethyl-2,2'-bipyridyl (Me) and 4,4'-dimethoxy-2,2'-bipyridine (MeO)) and 5,7-dibromo-8-quinolinoline derivatives (5,7-dibromo-2-methyl-8-quinolinol (MBrQ-H) and 5,7-dibromo-8-quinolinol (BrQ-H)) act as the chelating ligands. The in vitro cytotoxic activities of the five Ln(iii) complexes have been studied with the SK-OV-3/DDP, NCI-H460 and HeLa cancer cells. MeMBrQ-Lu, MeOMBrQ-Ho, MeMBrQ-Ho, MeBrQ-La and MeBrQ-Sm show higher cytotoxicity against the HeLa cells (IC50 values of 1.

In vitro and in vivo antitumor activities of three novel binuclear platinum(II) complexes with 4'-substituted-2,2':6',2″-terpyridine ligands.

Herein, we report the design and synthesis of three novel binuclear platinum(II) complexes, [Pt(tpbtpy)Cl][Pt(DMSO)Cl] (tpbtpy-Pt), [Pt(dthbtpy)Cl][Pt(DMSO)Cl]⋅CHOH (dthbtpy-Pt), and [Pt(qlbtpy)Cl][Pt(DMSO)Cl]⋅CHOH (qlbtpy-Pt) with 4'-(3-thiophenecarboxaldehyde)-2,2':6',2″-terpyridine (tpbtpy), 4'-(3,5-bis (1,1-dimethylethyl)-2-hydroxy-benzaldehyde)-2,2':6',2″-terpyridine (dthbtpy) and 4'-(2-quinolinecarboxaldehyde)-2,2':6',2″-terpyridine (qlbtpy) as ligands, respectively. All three novel binuclear platinum(II) complexes tpbtpy-Pt, dthbtpy-Pt, and qlbtpy-Pt were characterized by single-crystal X-ray diffraction analysis, spectroscopic analysis (ESI-MS, IR, H NMR), and elemental analysis. Additionally, the cytotoxicity of tpbtpy-Pt, dthbtpy-Pt and qlbtpy-Pt was assessed with human non-small cell lung cancer cell line (NCIH460 cells), yielding IC values in the range of 0.

Platinum(ii) complexes with rutaecarpine and tryptanthrin derivatives induce apoptosis by inhibiting telomerase activity and disrupting mitochondrial function.

Four new platinum(ii) complexes, [Pt(Rut)(DMSO)Cl] (), [Pt(Try)(DMSO)Cl] (), [Pt(ITry)(DMSO)Cl] () and [Pt(BrTry)(DMSO)Cl] (), with rutaecarpine (Rut), tryptanthrin (Try), 8-iodine-tryptanthrin (ITry) and 8-bromo-tryptanthrin (BrTry) as ligands were synthesized and fully characterized. In these complexes, the platinum(ii) adopts a four-coordinated square planar geometry. The inhibitory activity evaluated by the MTT assay showed that (IC = of 0.

Synthesis of two platinum(II) complexes with 2-methyl-8-quinolinol derivatives as ligands and study of their antitumor activities.

Two platinum(II) complexes, [Pt(ClQ)(DMSO)Cl] (ClQ-Pt) and [Pt(BrQ)(DMSO)Cl] (BrQ-Pt), with 5,7-dichloro-2-methyl-8-quinolinol (H-ClQ) and 5,7-dibromo-2-methyl-8-quinolinol (H-BrQ) as ligands, respectively, have been synthesized and characterized. The single-crystal X-ray diffraction characterization as well as other spectroscopic and analytical studies of ClQ-Pt and BrQ-Pt revealed that the coordination geometry of Pt(II) can be described as a four-coordinated square planar geometry. By MTT assay, ClQ-Pt displayed the most potent activity, with IC values of 5.

Synthesis and biological evaluation of substituted 3-(2'-benzimidazolyl)coumarin platinum(II) complexes as new telomerase inhibitors.

Eight new platinum(II) complexes Pt1-Pt8 with substituted 3‑(2'‑benzimidazolyl) coumarins were successfully synthesized and characterized by single crystal X-ray diffraction analysis, nuclear magnetic resonance spectroscopy (NMR), electrospray ionization-mass spectrometry (ESI-MS), infrared spectrophotometry (IR) and elemental analysis. Crystallographic data of these Pt1-Pt8 complexes showed that the Pt(II) has distorted four-coordinated square planar geometry. Pt1-Pt8 were found to display high cytotoxic activity in vitro against the cisplatin-resistant SK-OV-3/DDP cancer cells with a low IC from 1.

Novel tacrine platinum(II) complexes display high anticancer activity via inhibition of telomerase activity, dysfunction of mitochondria, and activation of the p53 signaling pathway.

In this work, we designed and synthesized tacrine platinum(II) complexes [PtClL(DMSO)]⋅CHOH (Pt1), [PtClL(DMP)] (Pt2), [PtClL(DPPTH)] (Pt3), [PtClL(PTH)] (Pt4), [PtClL(PIPTH)] (Pt5), [PtClL(PM)] (Pt6) and [PtClL(en)] (Pt7) with 4,4'-dimethyl-2,2'-bipyridine (DMP), 4,7-diphenyl-1,10-phenanthroline (DPPTH), 1,10-phenanthroline (PTH), 2-(1-pyrenecarboxaldehyde) imidazo [4,5-f]-[1,10] phenanthroline (PIPTH), 2-picolylamine (PM) and 1,2-ethylenediamine (en) as telomerase inhibitors and p53 activators. Biological evaluations demonstrated that Pt1Pt7 exhibited cytotoxic activity against the tested NCIH460, Hep-G2, SK-OV-3, SK-OV-3/DDP and MGC80-3 cancer cell lines, with Pt5 displaying the highest cytotoxicity. Pt5 exhibited an IC value of 0.

Synthesis, characterization and biological evaluation of six highly cytotoxic ruthenium(ii) complexes with 4'-substituted-2,2':6',2''-terpyridine.

Herein, six ruthenium(ii) terpyridine complexes, [RuCl(4-EtN-Phtpy)(DMSO)] (), [RuCl(4-MeO-Phtpy)(DMSO)] (), [RuCl(2-MeO-Phtpy)(DMSO)] (), [RuCl(3-MeO-Phtpy)(DMSO)] (), [RuCl(1-Bip-Phtpy)(DMSO)] (), and [RuCl(1-Pyr-Phtpy)(DMSO)] () with 4'-(4-diethylaminophenyl)-2,2':6',2''-terpyridine (4-EtN-Phtpy), 4'-(4-methoxyphenyl)-2,2':6',2''-terpyridine (4-MeO-Phtpy), 4'-(2-methoxyphenyl)-2,2':6',2''-terpyridine (2-MeO-Phtpy), 4'-(3-methoxyphenyl)-2,2':6',2''-terpyridine (3-MeO-Phtpy), 4'-(1-biphenylene)-2,2':6',2''-terpyridine (1-Bip-Phtpy), and 4'-(1-pyrene)-2,2':6',2''-terpyridine (1-Pyr-Phtpy), respectively, were synthesized and fully characterized. The MTT assay demonstrates that the anticancer activity of is higher than that of and more selective for Hep-G2 cells than for normal HL-7702 cells. In addition, various biological assays show that and , especially the complex, are telomerase inhibitors targeting c-myc G4 DNA and also cause apoptosis of Hep-G2 cells.

Synthesis and antitumor mechanisms of two novel platinum(ii) complexes with 3-(2'-benzimidazolyl)-7-methoxycoumarin.

Two novel platinum(ii) complexes, [PtCl2(H-MeOBC)(DMSO)] (Pt1) and [Pt2Cl3(MeOBC)(DMSO)2] (Pt2), with 3-(2'-benzimidazolyl)-8-methoxycoumarin (H-MeOBC) as the ligand were synthesized and evaluated for their antiproliferative activity. Among all the tumor cells, dual-Pt(ii) complex Pt2 exhibited the most potent activity, with an IC50 value of 0.5 ± 0.

Synthesis, Characterization, and Cytotoxicity of the Cobalt (III) Complex with N,N-Diethyl-4-(2,2':6',2''-terpyridin-4'-yl)aniline.

A cobalt(III) complex, [Co(L) ](ClO ) (1), in which the ligand L was N,N-diethyl-4-(2,2':6',2''-terpyridin-4'-yl)aniline (L), was synthesized and fully characterized. This new cobalt(III) complex 1 exhibited selective cytotoxicity against HeLa, T-24, A549, MGC80-3, HepG2, and SK-OV-3 cells with IC values in the micromolar range (0.52 - 4.

Synthesis, crystal structure and biological evaluation of a new dasatinib copper(II) complex as telomerase inhibitor.

A new copper(II) complex of dasatinib (DAS) was synthesized and characterized via ESI-MS, UV-Vis, IR, single-crystal X-ray diffraction analysis, H and C NMR spectroscopy, and elemental analysis. The composition of the new complex (1) was found to be [Cu(DAS + H)(NO)(HO)]NO·(HO)·(CHOH). Through MTT assay, it was found that 1 had high cytotoxicity towards A549, HeLa, BEL-7402, Hep-G2, NCI-H460, and MGC80-3 tumor cell lines, with IC values in 4.

Synthesis and in vitro biological evaluation of three 4'-(4-methoxyphenyl)-2,2':6',2″-terpyridine iridium(III) complexes as new telomerase inhibitors.

There iridium(III) complexes, [Ir(3-MeO-Phtpy)Cl] (1), [Ir(2-MeO-Phtpy)Cl] (2) and [Ir(4-MeO-Phtpy)Cl] (3) with 4'-(3-methoxyphenyl)-2,2':6',2″-terpyridine (3-MeO-Phtpy), 4'-(2-methoxyphenyl)-2,2':6',2″-terpyridine (2-MeO-Phtpy) and 4'-(4-methoxyphenyl)-2,2':6',2″-terpyridine (4-MeO-Phtpy) as ligands, respectively, were synthesized and evaluated for their antiproliferative activities. In these complexes, the iridium(III) center adopts a six-coordinate distorted octahedral geometry. Among them, complex 1 exhibited the most potent activity, with IC values of 3.