Janapala Venkateswara Rao

On water expedient synthesis of 3-indolyl-3-hydroxy oxindole derivatives and their anticancer activity in vitro.

A series of 3-indolyl-3-hydroxy oxindole derivatives (n = 41) were synthesized by the green aminocatalytic method with excellent yields under mild reaction conditions. All the newly synthesized derivatives were subjected to evaluate their cytotoxic properties against different human cancer cell lines. Results indicated that about 73% of the derivatives exhibited significant anti-proliferative activities against leukemia (U937, THP-1), lung (A549) and breast cancer (MCF7) cell lines. Among them a few of the derivatives exhibited the most potent and effective cytotoxic activities on U937 (34, 36, 38 and 41) and MCF7 (12, 35, 40 and 41) cell lines, and their anti-proliferation activities are better than the positive control, Etoposide.

New diterpenoids from Caesalpinia species and their cytotoxic activity.

Chemical investigation on Caesalpinia crista afforded two new diterpenoids, 6beta-cinnamoyloxy-7beta-acetoxyvouacapen-5alpha-ol and 6beta,7beta-dibenzoyloxyvouacapen-5alpha-ol and on Caesalpiniapulcherrima another new diterpenoid, 12-demethyl neocaesalpin F along with several known constituents. The structures of the new compounds were settled from their 1D and 2D NMR spectral data. The cytotoxicity of these compounds was measured on two different cancer cell lines.

Multifidone: a novel cytotoxic lathyrane-type diterpene having an unusual six-membered A ring from Jatropha multifida.

Chemical examination of the stems of Jatropha multifida afforded a novel lathyrane-type diterpene, multifidone, having an unusual six-membered A ring. The structure of the compound was determined from detailed analysis of its 1D and 2D NMR spectra and X-ray crystallographic analysis. Its cytotoxicity was measured on four different cancerous cell lines.

Synthesis of novel 1,2,3-triazole tagged pyrazolo[3,4-b]pyridine derivatives and their cytotoxic activity

A series of novel 1,2,3-triazole tagged pyrazolo[3,4-b]pyridine derivatives 3 and 4 were prepared respectively starting from 6-phenyl-4-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridin-3-amine 1 via selective N-propargylation, followed by reaction with diverse substituted alkyl/perfluoroalkyl/aryl/aryl amide azides under Sharpless conditions. All the synthesized compounds 3 and 4 were screened for cytotoxic activity against four human cancer cell lines such as U937, THP-1, HL60 and B16-F10. Compounds 3e, 4g, 4i and 4j which showed promising activity have been identified.

Synthesis and anti-mycobacterial activity of 2-chloronicotinaldehydes based novel 1H-1,2, 3-triazolylbenzohydrazides

1H-1,2,3-Triazolylbenzohydrazides (6a-h and 11a-l) were synthesized from 2-chloronicotinaldehydes and evaluated for anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv strain (ATCC-27294). Seven compounds 6b, 6e,f, 11d, 11h, 11j and 11l displayed potent anti-mycobacterial activity (MIC 2.8-6.2 μM). Potent anti-mycobacterial compounds were chosen for cytotoxicity studies by MTT protein assay against normal cell lines (PBMC and Raw 264.7) and shown low cytotoxicity. This is the first Letter assigning anti-mycobacterial activity, cytotoxicity and structure activity relationship for 1H-1,2,3-triazolylbenzohydrazides.

Profenofos induced biochemical alterations and in silico modelling of hatching enzyme, ZHE1 in zebrafish (Danio rerio) embryos.

The current study was aimed to investigate the oxidative stress response in zebrafish embryos exposed to sub-lethal (LC10) and lethal (LC50) concentrations of profenofos for 96-h and in silico modelling of zebrafish hatching enzyme, ZHE1 to explain the delayed hatching. Embryos exposed to profenofos under semi-static conditions significantly diminished glutathione (GSH), superoxide dismutase (SOD) and glutathione reductase (GR) levels, but increased the activities of catalase (CAT) and glutathione S-transferase (GST) concomitantly with marked elevation in malondialdehyde (MDA) content in whole-body homogenate of the treated groups compared with control. In addition, stress protein Hsp70 expression and DNA damage were significantly increased in a concentration- dependent manner compared with controls. From the computational docking studies of ZHE1 with profenofos revealed that profenofos is binding to three amino acids, histidine 99, histidine 109 and arginine 182 at the active site of the enzyme through hydrogen bonding which may lead to inhibition of hatching.

Studies on Synthesis of Novel Triazolalkyl Tagged Trifluoromethyl Substituted Pyrimidine Derivatives and their Evaluation for Cytotoxic Activity

The 2-amino-6-trifluoromethyl-3H-pyrimidin-4-one 1 was propargylated to give two regioisomers 2, 3 in defi- nite proportions. Both regioisomers 2 and 3 were independently reacted with alkyl, aryl or cycloalkyl substituted azides under Sharpless conditions and were obtained exclusively 1,4-disubstituted triazole tagged trifluoromethyl substituted pyrimidine derivatives 4 and 5 respectively. All the final products were evaluated for cytotoxic activity against four can- cer cell lines and promising compounds were identified.