Design and Synthesis of Various Aryl Amide Derivatives of Imidazo[1,5-a] Pyridine-1,2,4-Thiadiazoles: In Vitro Cytotoxicity Evaluation and In Silico Molecular Docking Studies.

A new series of various aryl amide derivatives of imidazo[1,5-a]pyridine-1,2,4-thiadiazoles (15a-j) were designed, synthesized, and evaluated for their cytotoxic profiles against four human cancer cell lines such as breast cancer (MCF-7), lung cancer (A549), colon cancer (Colo-205), and ovarian cancer (A2780), via the MTT assay, with etoposide as the standard known chemotherapeutic agent. Five compounds, 15a, 15b, 15c, 15f, and 15j, exhibited more potent cytotoxic effects than did etoposide. Among them, compound 15a exhibited potent cytotoxic effects against the MCF-7, A549, Colo-205, and A2780 cell lines, with IC values of 0.

Design, Synthesis, and Biological Evaluation of 1,2,4-Thiadiazole-1,2,4-Triazole Derivatives Bearing Amide Functionality as Anticancer Agents.

A novel library of amide functionality having 1,2,4-thiadiazole-1,2,4-triazole () analogs was designed, synthesized, and structures were characterized by H NMR, C NMR, and mass (ESI-MS) spectral data. Further, all compounds were evaluated for their anticancer activities against four different cancer cell lines including breast cancer (MCF-7, MDA MB-231), lung cancer (A549), and prostate cancer (DU-145) by MTT reduction assay method, and etoposide acts as a standard drug. The results confirmed that majority of the synthesized compounds showed moderate to potent anticancer activities aligned with four cell lines.

Stereoselective total synthesis of Patulolide C.

Stereoselective total synthesis of Patulolide C has been accomplished from easily available and inexpensive ()chiral epoxide. The key steps involved in the concise synthesis of Patulolide C utilizes ring opening of chiral epoxide, cleavage of 1,2-diol, deprotection of benzyl ether of hydroxyl acid and Yamaguchi macrolactonisation dilution conditions as key steps. The advantage of this method include inexpensive starting material, mild reaction conditions and high purity of products.

Synthesis, antiproliferative and apoptosis induction potential activities of novel bis(indolyl)hydrazide-hydrazone derivatives.

In recent years, indole-indazolyl hydrazide-hydrazone derivatives with strong cell growth inhibition and apoptosis induction characteristics are being strongly screened for their cancer chemo-preventive potential. In the present study, N-methyl and N,N-dimethyl bis(indolyl)hydrazide-hydrazone analog derivatives were designed, synthesized and allowed to evaluate for their anti-proliferative and apoptosis induction potential against cervical (HeLa), breast (MCF-7 and MDA-MB-231) and lung (A549) cancer cell lines relative to normal HEK293 cells. The MTT assay in conjunction with mitochondrial potential assays and the trypan blue dye exclusion were employed to ascertain the effects of the derivatives on the cancer cells.

An alternative stereoselective total synthesis of (-)-pyrenophorol.

The total synthesis of 16-membered C-Symmetric dilactone (-)-Pyrenophorol was accomplished starting from commercially available ()epoxide prepared by hydrolytic kinetic resolution of (±) - epoxide with key steps of Grignard reaction, Swern oxidation, Wittig reaction and cyclization was achieved by intermolecular Mitsunobu cyclization. The synthesis of (-)-Pyrenophorol accomplished from cheaply available starting material, easily work-up procedures and reduction of cost in industrial process were major advantages of this route.

Synthesis of chalcone incorporated quinazoline derivatives as anticancer agents.

A series of ten novel chalcone incorporated quinazoline derivatives (-) were designed and synthesized. All the synthesized compounds were evaluated for their anticancer activities against four human cancer cell lines (A549, HT-29, MCF-7 and A375). Among them, four compounds, , , and showed more potent anticancer activity than the control drug, Combretastatin - A4.