Bi(OTf)3 PROMOTED MICROWAVE SYNTHESIS OF 2-ARYL, 5-SUBSTITUTED 1,3,4-OXADIAZOLES AND EVALUATION OF THEIR ANTICANCER ACTIVITY

Synthesis and anticancer activity of novel 5-(indole-2-yl)-3-substituted 1,2,4-oxadiazoles.

A new series of 5-(indole-2-yl)-3-substituted 1,2,4-oxadiazoles were synthesized and evaluated for their anticancer activities. Structures of the compounds were confirmed by spectroscopic methods. Structural modifications were done to improve the antiproliferative activity of compound 1. The results indicated that a benzyloxyl substituent on the C-4 position was better than a methyl substituent...

Synthesis and Anticancer Activity of N-Aryl-5-substituted-1,3,4-oxadiazol-2-amine Analogues

In continuance of our search for anticancer agents, we report herein the synthesis and anticancer activity of some novel oxadiazole analogues. The compounds were screened for anticancer activity as per National Cancer Institute (NCI US) protocol on leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancers cell lines. N-(2,4-Dimethylphenyl)-5-(4-methoxyphenyl)-1,3,4-oxad...

Propylphosphonic anhydride (T3P) mediated synthesis of novel 2-aryl quiolines and evaluation of their anticancer activity

Synthesis of 5-substituted 2'-deoxyuridine-5'- phosphonate analogues and evaluation of their antiviral activity.

A small series of 5-(hetero)aryl-modified nucleoside phosphonates was synthesized via an 8-step procedure including a Wittig reaction and Suzuki-Miyaura coupling. An unanticipated anomerization during phosphonate deprotection allowed us to isolate both anomers of the 5-substituted 2'-deoxy-uridine phosphonates and assess their antiviral activity against a broad panel of viruses.

Design, Synthesis and Evaluation of Substituted Aryl-2-Nitrovinyl Derivatives as Small Molecules Proteasome Inhibitors

Based on the existing structure activity relationship for proteasome inhibitors, a number of substituted aryl-2-nitrovinyl derivatives have been synthesized as Michael acceptor and their cytotoxicity and proteasome inhibitory effects were evaluated on two cancer cell lines. Compound 2d exhibited IC50 values of 0.71 and 17.79 μM comparable to bortezomib against MCF-7 and PC-3, respectively. The ...