Synthesis of new triazole fused imidazo[2,1-b]thiazole hybrids with emphasis on Staphylococcus aureus virulence factors.

A series of new triazole fused imidazo[2,1-b]thiazole hybrids (9a-u) were designed, synthesized and evaluated as antimicrobial agents. Compounds 9c, 9d, 9e, 9j and 9l showed promising broad spectrum antimicrobial activity. Further, compound 9c exhibited significant anti-biofilm activity with single and mixed biofilm disruption demonstrated by Field Emission Scanning Electron Microscope (FE-SEM).

Design, synthesis, and antimicrobial evaluation of 1,4-dihydroindeno[1,2-]pyrazole tethered carbohydrazide hybrids: exploring their ADMET, ergosterol inhibition and ROS inducing potential.

A series of new 1,4-dihydroindeno[1,2-]pyrazole tethered carbohydrazide hybrids () were designed, synthesized and evaluated for their antimicrobial activity. Compounds , , , and demonstrated significant activity against the entire panel of test pathogens. Further, compounds and exhibited significant anti- activity.

Click chemistry-assisted synthesis of triazolo linked podophyllotoxin conjugates as tubulin polymerization inhibitors.

A series of new triazolo linked 4β-amidopodophyllotoxin conjugates () were synthesized using click chemistry and evaluated for their antitumor activity against four human cancer cell lines. Among them, two compounds ( and ) showed significant anticancer activity with IC values of 0.9 and 0.

Imidazopyridine linked triazoles as tubulin inhibitors, effectively triggering apoptosis in lung cancer cell line.

A library of new imidazopyridine linked triazole hybrid conjugates (8a-r) were designed, synthesized and evaluated for their cytotoxicity against four cancer cell lines namely, human lung (A549), human prostate (DU-145), human colon (HCT-116) and breast (MDA-MB 231) cancer. These conjugates exhibited good to moderate activity against the tested human cancer cell lines. Two of the conjugates (8g and 8j) showed significant antitumor activity against human lung cancer cell line (A549) with IC values of 0.

Development of pyrrolo[2,1-c][1,4]benzodiazepine β-glucoside prodrugs for selective therapy of cancer.

Cancer chemotherapy has several limitations such as often insufficient differentiation between malign tissue and benign tissue. The clinical utility of the pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) are inadequate because of the lack of selectivity for tumor tissues, high reactivity of the pharmacophoric imine functionality, low water solubility, and stability. To address these limitations two new β-glucoside prodrugs of PBDs have been synthesized and evaluated for their potential use in selective therapy of solid tumors by ADEPT.

Design, synthesis and biological evaluation of imidazopyridine-propenone conjugates as potent tubulin inhibitors.

A library of imidazopyridine-propenone conjugates () were synthesized and evaluated for their antitumor activity against four human cancer cell lines, namely, prostate (DU-145), lung (A549), cervical (Hela) and breast (MCF-7) cancer cell lines. These conjugates showed good to moderate activity against the tested cell lines. Among them, two conjugates ( and ) showed significant antiproliferative activity against the human lung cancer cell line (A549) with IC values of 0.

Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.

A series of phenstatin/isocombretastatin-oxindole conjugates was synthesized and tested for their cytotoxic activity against five human cancer cells such as prostate (DU-145), lung (A549), colon (HT-29), breast (MCF-7), liver (HepG2) cancer cells with IC50 values ranging from 0.049 to 38.90 μM.