Discovery of dual-targeted molecules based on Olaparib and Rigosertib for triple-negative breast cancer with wild-type BRCA.

PARP inhibitors (PARPis) demonstrate significant potential efficacy in the clinical treatment of BRCA-mutated triple-negative breast cancer (TNBC). However, a majority of patients with TNBC do not possess BRCA mutations, and therefore cannot benefit from PARPis. Previous studies on multi-targeted molecules derived from PARPis or disruptors of RAF-RAF pathway have offered an alternative approach to develop novel anti-TNBC agents.

Foegraecumoside O and P, a Pair of Triterpenoid Saponins with a 4/5/6 Fused Tricyclic Oleanane Carbon Skeleton from Hance.

Hance (Primulaceae) is a medicinal plant used for cold, pain, ascariasis, etc., in China. Triterpenoid saponins have been found to be the main components of this genus.

Antitumor activity and mechanisms of dual EGFR/DNA-targeting strategy for the treatment of lung cancer with EGFR mutation.

Dual- or multi-targeted EGFR inhibitors as single drugs can overcome EGFR inhibitor resistance and circumvent many disadvantages of combination therapy. In this work, fifteen 4-anilinoquinazoline derivatives bearing nitrogen mustard or hemi mustard moieties were designed and synthesized as dual EGFR-DNA targeting anticancer agents. Structures of target molecules were confirmed by H NMR, C NMR and HR-MS, and evaluated for their in vitro anti-proliferative activities using MTT assay.

(±)-Corysaxicolaine A: a pair of antitumor enantiomeric alkaloid dimers from .

(±)-Corysaxicolaine A (1), isolated from the aerial parts of for the first time, is a pair of novel dimeric alkaloids, each of which is directly coupled by the rare 6, 12' C-C σ-bond between benzophenanthridine and protoberberine. The enantiomeric separation was achieved using chiral chromatography. Their structures, including stereochemistry, were clarified by carrying out extensive spectroscopic techniques and an electronic circular dichroism (ECD) calculation.

Extraction optimization, physicochemical characterization, and antioxidant activity of polysaccharides from sp. SCSIO-45730.

Unlabelled: Microalgal polysaccharides have been reported in many studies due to their uniqueness, biocompatibility, and high value, and sp. SCSIO-45730 was an excellent source of polysaccharides and β-glucans. However, the polysaccharides from the red unicellular alga sp.

Platinum(IV) complexes conjugated with chalcone analogs as dual targeting anticancer agents: In vitro and in vivo studies.

For the sake to develop novel platinum(IV) complexes to reverse cisplatin (CDDP) resistence, four multifunctional platinum(IV) prodrugs via conjugating chalcones with the related platinum(IV) complexes derived from cisplatin were designed and evaluated for anti-tumor actyivities in vitro and in vivo. Among them, complex 9 exhibited excellent anticancer activities in vitro with IC values at the submicromolar level against the tested human cancer cells, whereas showed low cytotoxicity towards human normal liver cells HL-7702. Further mechanistic studies indicated that complex 9 induced G2/M phase arrest and apoptosis in A549 cells, which was associated with a collapse of the mitochondrial membrane potential (MMP), alterations in the expression of some apoptosis-related proteins, and enhanced level of the intracellular reactive oxygen species (ROS).

Mitochondria-targeted triphenylphosphonium conjugated glycyrrhetinic acid derivatives as potent anticancer drugs.

Glycyrrhetinic acid has been usually studied for their anti-tumor activities. However, the low bioavailability and poor aqueous solubility as well as limited intracellular accumulation have limited their utility. In this present study, a series of new glycyrrhetinic acid conjugates with a triphenylphosphonium cation (TTP) moiety, meant to specifically target them to tumor cells mitochondria, have been designed and synthesized.

[Studies on chemical constituents of Clerodendrum bungei].

Ten compounds were isolated from the 95% aqueous EtOH extract of Clerodendrum bungei by a combination of various chromatographic techniques including column chromatography over silica gel, Sephadex LH-20, MCI, ODS, and semi-preparative HPLC. Their structures were elucidated as 11,12,16S-trihydroxy-7-oxo-17(15→16),18(4→3)-diabeo-abieta-3,8,11,13-tetraen-18-oic acid (1), 12S*,13R*-dihydroxy-9-oxo-octadeca-10(E)-enoic acid (2), clerodenoside A (3), trichotomoside (4), glycosmisic acid (5), 4'-O-methylscutellarein (6), neroplomacrol (7), butylitaconic acid (8), hexylitaconic acid (9), p-hydroxybenzonic acid (10) by their physicochemical properties and spectroscopic data. Compounds 1 and 2 are new natural products, while compounds 7-10 were obtained from the genus Clerodendrum for the first time, and compounds 3, 5, 6 were isolated from this plant for the first time.

Mappianines A-E, structurally diverse monoterpenoid indole alkaloids from Mappianthus iodoides.

Five previously undescribed monoterpenoid indole alkaloids, mappianines A-E, along with twelve known analogues, were isolated from the stems of Mappianthus iodoides Hand.-Mazz. Their structures and absolute configurations were determined by spectroscopic analysis, single-crystal X-ray diffraction, and ECD calculations.

Cytotoxic triterpenoid saponins from Lysimachia foenum-graecum.

Eleven oleanane-type triterpenoid saponins, foegraecumosides A-K, and eight known ones, were isolated from the aerial parts of Lysimachia foenum-graecum. Their structures were elucidated by spectroscopic data analyses and chemical methods. All isolated saponins were evaluated for their cytotoxicity against four human cancer cell lines (NCI-H460, MGC-803, HepG2, and T24).

Antitumor lignanamides from the aerial parts of Corydalis saxicola.

Background: Cancer is one of the leading cause of unnatural death globally. There is still a great need for effective anticancer agents from plant sources. Corydalis saxicola Bunting is a medicinal plant that is traditionally used to treat various diseases in southwest China.