Sulfonyl-acetohydrazide derivatives as juvenile hormone mimics to be insect growth regulators.

The need for targeted pest control strategies has led to the development of juvenile hormone (JH) mimics that selectively disrupt the life cycles of harmful insect species. Present study focuses on the synthesis, characterization and evaluation of sulfonyl-acetohydrazide derivatives (H1-H8) as novel JH mimics on two different insect species, with an emphasis on their insect-specific action. The yellow fever mosquito, Aedes aegypti and cabbage leaf borer, Spodoptera litura, were selected for this investigation.

A Comprehensive Review on the Development of Titanium Complexes as Cytotoxic Agents.

After the discovery of cis-platin, the first metal-based anticancer drugs, budotitane, and titanocene dichloride entered clinical trials. These two classes of complexes were effective against those cell lines that are resistant to cis-platin and other platinum-based drugs. However, the main limitation of these complexes is their low hydrolytic stability.

Juvenile hormone mimics with phenyl ether and amide functionality to be insect growth regulators (IGRs): synthesis, characterization, computational and biological study.

A series of substituted phenyl ethers derivatives as juvenile hormone (JH) mimics (V-V) have been synthesized. Substituted phenoxyacetic acid and amino acid ethyl ester hydrochloride were prepared using NaOH, SOCl. DCC method has been used for amide linkage.

Isoleucine with secondary sulfonamide functionality as anticancer, antibacterial and antifungal agents.

Isoleucine substituted analogues with secondary sulfonamide group (I-I) have been synthesized. Structures of synthesized analogues have been confirmed by Fourier Transform-Infrared Red, Nuclear Magnetic Resonance (H and C) and ESI-MS spectroscopic tools. Cytotoxic screenings of synthesized analogues have been done on MCF-7 (breast), Prostate Cancer-3 (PC-3) and A549 (lung) cancer cell lines.

Sulfonamide phenylalanine (SPA) series of analogues as an antibacterial, antifungal, anticancer agents along with p53 tumor suppressor-DNA complex inhibitor - part 1.

A series of N-[1-benzyl-2-oxo-2-substituted(ethyl)] benzene/-toluene sulfonamide (K1-K12) are synthesized. Structure of the synthesized analogues has been confirmed by FT-IR, H & C NMR and ESI-MS spectroscopic techniques. All the synthesized analogues (K1-K12) have also been examined for their antibacterial and antifungal activities.

Structural and biological study of synthesized anthraquinone series of compounds with sulfonamide feature.

1, 4 and 5, 8-Positions as well as type of functionalities on these positions at anthraquinone-9, 10-dione are proposed to be significant for anticancer activity. Therefore, keeping this into consideration, a series of 1-substituted anthraquinone-based compounds are designed, synthesized, characterized and biologically evaluated for anticancer activity. The structure of synthesized compounds is confirmed by spectroscopic analysis, i.

Synthesis, Spectral Characterization, Antibacterial and Anticancer Activity of some Titanium Complexes.

Background: After the discovery of cisplatin, first non platinum anticancer drugs having excellent efficacy were budotitane and TiCl2(cp)2 but action mechanism is not clear. Therefore, we hereby reporting synthesis and biological activities novel titanium complexes to explore their mode of action.

Objectives: Synthesis, spectral characterization, antibacterial and anticancer activity of some titanium complexes.

In silico and bio assay of juvenile hormone analogs as an insect growth regulator against Galleria mellonella (wax moth) - Part I.

Juvenile hormone (JH) analogs are nowadays in use to control harmful pests. In order to develop new bioactive molecules as potential pesticides, we have incorporated different active structural features like sulfonamide, aromatic rings, amide group, and amino acid moiety to the base structure. We have screened a series of designed novel JH analogs against JH receptor protein (jhbpGm-2RCK) of Galleria mellonella in comparison to commercial insect growth regulators (IGRs) - Pyriproxyfen (T1) and Fenoxycarb (T2).

Comparative In Vitro Binding Studies of TiCl2(dpme)2, Ti(ada)2(bzac)2, and TiCl2(bzac)(bpme) Titanium Complexes with Calf-Thymus DNA.

The binding of TiCl2(dpme)2 (1), (dpme = 6,6'-dimethyl-2,2'-bipyridine), Ti(ada)2(bzac)2 (2), (ada = adamantylamine; bzac = benzoylacetone), and TiCl2(bzac)(bpme) (3), (bpme = 4,4'-dimethyl-2,2'-bipyrdine) with calf thymus (ct) DNA has been studied by UV-visible spectroscopy, thermal denaturation, and circular dichroism spectroscopy. In UV-visible study complexes 1, 2, and 3 showed red, blue, and red shifts, respectively, upon the addition of ct-DNA along with a significant hyperchromism. The intrinsic binding constants (K b ) calculated from UV-visible absorption studies were 2.

Synthesis, Characterization, Biological Evaluation and Docking Study of Heterocyclic-Based Synthetic Sulfonamides as Potential Pesticide Against G. mellonella.

Juvenile hormone is an important hormone which controls the developmental process in the lepidopteran insects, hence, referred as insect growth regulator. Juvenile hormone binding proteins are the carrier of juvenile hormone from the site of secretion to the site of action and play vital role in juvenile hormone action. We have designed four different juvenile hormone analogs incorporating sulfonamide and heterocyclic moieties using computer-aided tools.

Synthesis, spectral characterization, and antiproliferative studies of mixed ligand titanium complexes of adamantylamine.

Titanium complexes have been synthesized by the reaction between titanium tetrachloride (TiCl4), respective bidentate ligand [4,4' -dimethoxy-2,2' -bipyridine (bpome), 6,6'-dimethyl-2,2'-bipyridine (dpme), 1,2-diaminocyclohexane (dach), 1,10-phenanthroline (phen), and benzoylacetone (bzac)], and adamantylamine (ada) in 1 : 2 : 2 molar ratios, respectively. The structure of synthesized complexes was confirmed using elemental analysis, FTIR, UV-visible, (1)H NMR, and mass spectrometry techniques. The nanocrystalline nature of complexes was confirmed by powder XRD study.

Multispectroscopic methods reveal different modes of interaction of anti cancer drug mitoxantrone with Poly(dG-dC).Poly(dG-dC) and Poly(dA-dT).Poly(dA-dT).

The interaction of mitoxantrone with alternating Poly(dG-dC).Poly(dG-dC) and Poly(dA-dT).Poly(dA-dT) duplex has been studied by absorption, fluorescence and Circular Dichroism (CD) spectroscopy at Drug to Phosphate base pair ratios D/P=20.

NMR-based structure of anticancer drug mitoxantrone stacked with terminal base pair of DNA hexamer sequence d-(ATCGAT)2.

Mitoxantrone is a promising antitumor drug having considerably reduced cardiotoxicity as compared to anthracyclines. Its binding to deoxyhexanucleotides sequence d-(ATCGAT)2 has been studied by proton and phosphorous-31 nuclear magnetic resonance spectroscopy. The stoichiometry reveals that 1:1 and 2:1 mitoxantrone-d(ATCGAT)2 complexes are formed in solution.

Interaction of anticancer drug mitoxantrone with DNA hexamer sequence d-(CTCGAG)2 by absorption, fluorescence and circular dichroism spectroscopy.

The interaction of mitoxantrone with d-(CTCGAG)2 has been studied by absorption, fluorescence and circular dichroism (CD) spectroscopy. The hypochromism and quenching of fluorescence showed that about four mitoxantrone molecules may be binding externally to DNA hexamer sequence at high drug to nucleic (D/N) acid duplex ratios (28.0-1.

Molecular modeling study of interaction of anthracenedione class of drug mitoxantrone and its analogs with DNA tetrameric sequences.

Numbers of drugs are being synthesized every year to meet the target of safe and disease-free society. Presently molecular modeling technique is used to unfold the mechanism of action of drugs alone or in conjunction with experimental methodologies. There are a number of drugs which are successfully developed using this methodology.

Structure of daunomycin complexed to d-TGATCA by two-dimensional nuclear magnetic resonance spectroscopy.

The anthracycline antibiotic daunomycin, having four fused rings and an amino sugar, is being used in the treatment of acute leukemia. Binding to DNA is generally believed to be essential for its activity. We have studied the interaction of daunomycin with DNA hexamer sequence d-(TGATCA)2 by titrating up to two drug molecules per duplex using nuclear magnetic resonance spectroscopy.

Structure of DNA sequence d-TGATCA by two-dimensional nuclear magnetic resonance spectroscopy and restrained molecular dynamics.

The 5' d-TpG 3' element is a part of DNA sequences involved in regulation of gene expression and is also a site for intercalation of several anticancer drugs. Solution conformation of DNA duplex d-TGATCA containing this element has been investigated by two-dimensional NMR spectroscopy. Using a total of 12 torsional angles and 121 distance constraints, structural refinement has been carried out by restrained molecular dynamics (rMDs) in vacuum up to 100 ps.

Structure of DNA hexamer sequence d-CGATCG by two-dimensional nuclear magnetic resonance spectroscopy and restrained molecular dynamics.

Solution conformation of self-complementary DNA duplex d-CGATCG, containing 5' d-CpG 3' site for intercalation of anticancer drug, daunomycin and adriamycin, has been investigated by nuclear magnetic resonance (NMR) spectroscopy. Complete resonance assignments of all the protons (except some H5'/H5" protons) have been obtained following standard procedures based on double quantum filtered correlation spectroscopy (dQF COSY) and two-dimensional nuclear Overhauser effect (NOE) spectra. Analysis of sums of coupling constants in one-dimensional NMR spectra, cross peak patterns in dQF COSY spectra and inter proton distances shows that the DNA sequence assumes a conformation close to the B-DNA family.