title: Synthesis and biological screening of 5-(alkyl(1H-indol-3-yl))-2-(substituted)-1,3,4-oxadiazoles as antiproliferative and anti-inflammatory agents.
abstract: A series of 5-(alkyl(1H-indol-3-yl))-2-(substituted)-1,3,4-oxadiazoles were efficiently synthesized by oxidative cyclisation of N'-benzylidene-(1H-indol-3-yl)alkane hydrazides using di(acetoxy)iodobenzene. N'-Benzylidene-(1H-indol-3-yl)alkane hydrazides themselves were derived from simple indole-3-carboxylic acids. The 5-(alkyl(1H-indol-3-yl))-2-(substituted)-1,3,4-oxadiazoles were evaluated for their anti-inflammatory and anti-proliferative activities. Based on the results obtained structure and activity relationship (SAR) was established and a correlation between the activities was observed. Compound 6i and 6t showed best activity against proliferation of human cancer cell lines and as well as inflammation of rat paw edema.
authors.affiliation: Crop Protection Chemicals Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500607, India.
authors.forename: Sreevani
authors.initials: S
authors.lastname: Rapolu
authors.forename: Manjula
authors.initials: M
authors.lastname: Alla
authors.forename: Vittal Rao
authors.initials: VR
authors.lastname: Bommena
authors.forename: Ramalinga
authors.initials: R
authors.lastname: Murthy
authors.forename: Nishant
authors.initials: N
authors.lastname: Jain
authors.forename: Venkata Ramya
authors.initials: VR
authors.lastname: Bommareddy
authors.forename: Madhava Reddy
authors.initials: MR
authors.lastname: Bommineni
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008297:Male; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D010069:Oxadiazoles
keywords: Anti-inflammatory agents; Antiproliferative agents; Indole-3-carboxlic acids; Indolyl-1,3,4-oxadiazoles