Department of Chemistry
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Item Synthesis and anticancer activities of novel 3,5-disubstituted-1,2,4-oxadiazoles(Elsiever, 2009-05) Kumar, DalipA series of 3,5-disubstituted-1,2,4-oxadiazoles were synthesized and evaluated for their in vitro anti-proliferative activities against various cancer cell lines. Formation of 1,2,4-oxadiazole ring was accomplished by the reaction of amidoxime with carboxylic acids. The in vitro cytotoxic effects of 3,5-disubstituted-1,2,4-oxadiazoles have been demonstrated across a wide array of tumor cell types and a few compounds exhibited specificity towards pancreatic (3f, 3h, 3j, and 3k) and prostate (3n) cancer cells. Among the prepared 3,5-disubstituted-1,2,4-oxadiazoles, compound 3n is the most selective (>450-fold) and compound 3p is the most cytotoxic (10 nM) against prostate cancer cell lines.Item Novel porphyrin–psoralen conjugates: synthesis, DNA interaction and cytotoxicity studies(CBI, 2013) Kumar, DalipThe indole ring system is the most privileged heterocycle in nature and embedded in many biological systems. The demonstration of many indole containing alkaloids as leads for the new pharmaceutical agents, the recognition of the importance of essential amino acid tryptophan in human nutrition and the discovery of plant hormones served to bring about a massive search on indole chemistry. This led to report vast number of structurally diversified bio-active natural and synthetic indoles. The present review focuses on the structure-based drug design of variety of classes of synthetic indoles as potent anticancer agents. Particularly, the recent developments on natural-product inspired rational synthesis of functionalized indoles, indolylazoles and bis(indoles) and their anticancer activities are presented. This review also drawn the attention towards combretastatin-based structural class of indoles and well discussed their potentials as tubulin polymerization inhibitorsItem Synthesis and anticancer activity study of indolyl hydrazide–hydrazones(Springer, 2016-03-03) Kumar, DalipA series of N′-((1-(substituted)-1H-indol-3-yl)methylene)hydrazides were synthesized and evaluated for their in vitro antiproliferative activities against various cancer cell lines. Formation of indole hydrazide–hydrazones was accomplished by the reaction of indole 3-carboxaldehyde with aryl/alkyl hydrazides in the presence of acetic acid. Out of synthesized twenty-two compounds, some of the analogs exhibited specificity toward breast (18b, 18d, 18f and 18j) and prostate (18t and 18v) cancer cells. Among the prepared derivatives, compounds 18b, 18d and 18j were most cytotoxic (IC50 = 0.9, 0.4 and 0.8 µM, respectively) against the screened cancer cell lines. Exposure of PC3 cells to either 18d or 18j resulted in increased levels of cleaved PARP1, indicating that indolyl hydrazide–hydrazones induce apoptosis in PC3 cells.Item Synthesis and biological evaluation of novel carbazolyl glyoxamides as anticancer and antibacterial agents(RSC, 2016) Kumar, DalipA new library of 24 carbazolyl glyoxamides 14a–x were designed and synthesized from glyoxalic acids and arylamines in the presence of HATU as a coupling reagent under MW irradiation. The synthesized carbazolyl glyoxamides were evaluated for their in vitro anticancer and antibacterial activities. Of the synthesized carbazolyl glyoxamides, compounds 14l and 14q exhibited the most potent cytotoxicity towards a breast cancer cell line with IC50 values of 9.3 and 9.8 μM, respectively. Further, caspase-3 assay for carbazolyl glyoxamides indicated that these compounds induced apoptotic cell death in Jurkat cells. Furthermore, some of the synthesized carbazolyl glyoxamides 14g, 14k, 14l and 14n exhibited comparable or even better antibacterial activity (MIC = 8–16 μg mL−1) than chloramphenicol against the selected bacterial strainsItem One-pot synthesis and in-vitro anticancer evaluation of 5-(2′-indolyl)thiazoles(Springer Nature, 2016-03-29) Kumar, DalipA series of 5-(2′-indolyl)thiazoles were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of thioamides 3 with 3-tosyloxypentane-2,4-dione 4 led to in situ formation of 5-acetylthiazole 5 which upon treatment with arylhydrazines 6 in polyphosphoric acid resulted in the formation of 5-(2′-indolyl)thiazoles 2. Among the synthesized 5-(2′-indolyl)thiazoles, compounds 2d–f and 2h exhibited encouraging anticancer activity and also selectivity towards particular cell lines (IC50 = 10–30 μM). Further studies on the SAR of compound 2e may result in good anticancer activity.Item Synthesis and anticancer activity studies of indolylisoxazoline analogues(PMC, 2018-07-26) Kumar, Anil; Kumar, DalipA new library of thirteen indolylisoxazolines 6a-m has been synthesized by the treatment of indolylchalcones with hydroxylamine hydrochloride. Evaluation of anticancer activity of indolylisoxazolines 6a-m led to the identification of potent compounds 6c-d, 6i and 6l, with IC50 ranging 2.5-5.0 µM against the tested cancer cell lines. Using a number of complementary techniques such as acridine orange/ethidium bromide staining, PARP1 cleavage and DNA strand breaks assay, we show that the compounds 6c and 6i induce apoptosis in highly aggressive C4-2 cells. Our data further revealed that 6c and 6i inhibited C4-2 cells proliferation without inducing reactive oxygen species (ROS). Finally, we show that compounds 6c and 6i also potently inhibit cell migration, indicating these compounds have the potential to serve as effective anti-cancer agents.