BIOMAT Database Logo BIOMAT Database Logo

Synthesis of new secretory phospholipase A2-inhibitory indole containing isoxazole derivatives as anti-inflammatory and anticancer agents. 2016

Srinivasa Rao Pedada, and Nagendra Sastry Yarla, and Pawan J Tambade, and Bhadrapura Lakkappa Dhananjaya, and Anupam Bishayee, and Kalle M Arunasree, and Gundala Harold Philip, and Gangappa Dharmapuri, and Gjumrach Aliev, and Swathi Putta, and Gururaja Rangaiah
Centre for Research and Development, PRIST University, Thanjavur 613 403, Tamilnadu, India.

Secretory phospholipase A2 (sPLA2) is an important enzyme that plays a key role in various inflammatory diseases including cancer and its inhibitors have been developed as preventive or therapeutic agents. In the present study, a series of new indole containing isoxazole derivatives (10a-10o) is synthesized and evaluated for their sPLA2 inhibitory activities. All compounds (10a-10o) showed significant sPLA2 inhibition activities both in vitro and in vivo studies which is substantiated in in silico studies. Among all the tested compounds, 10o showed potent sPLA2 inhibition activity, that is comparable or more to ursolic acid (positive control). Further studies demonstrated that 10o showed in vitro antiproliferative activity when tested against MCF-7 breast and DU145 prostate cancer cells. Furthermore, compounds 10a-10o obeyed lipinsky's rule of 5 and suggesting druggable properties. The in vitro, in vivo and in silico results are encouraging and warrant pre-clinical studies to develop sPLA2-inhibitory compound 10o as novel therapeutic agent for various inflammatory disorders and several malignancies.

UI MeSH Term Description Entries
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D007555 Isoxazoles Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions. Isoxazole
D008297 Male Males
D008958 Models, Molecular Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures. Molecular Models,Model, Molecular,Molecular Model
D011471 Prostatic Neoplasms Tumors or cancer of the PROSTATE. Cancer of Prostate,Prostate Cancer,Cancer of the Prostate,Neoplasms, Prostate,Neoplasms, Prostatic,Prostate Neoplasms,Prostatic Cancer,Cancer, Prostate,Cancer, Prostatic,Cancers, Prostate,Cancers, Prostatic,Neoplasm, Prostate,Neoplasm, Prostatic,Prostate Cancers,Prostate Neoplasm,Prostatic Cancers,Prostatic Neoplasm
D001943 Breast Neoplasms Tumors or cancer of the human BREAST. Breast Cancer,Breast Tumors,Cancer of Breast,Breast Carcinoma,Cancer of the Breast,Human Mammary Carcinoma,Malignant Neoplasm of Breast,Malignant Tumor of Breast,Mammary Cancer,Mammary Carcinoma, Human,Mammary Neoplasm, Human,Mammary Neoplasms, Human,Neoplasms, Breast,Tumors, Breast,Breast Carcinomas,Breast Malignant Neoplasm,Breast Malignant Neoplasms,Breast Malignant Tumor,Breast Malignant Tumors,Breast Neoplasm,Breast Tumor,Cancer, Breast,Cancer, Mammary,Cancers, Mammary,Carcinoma, Breast,Carcinoma, Human Mammary,Carcinomas, Breast,Carcinomas, Human Mammary,Human Mammary Carcinomas,Human Mammary Neoplasm,Human Mammary Neoplasms,Mammary Cancers,Mammary Carcinomas, Human,Neoplasm, Breast,Neoplasm, Human Mammary,Neoplasms, Human Mammary,Tumor, Breast
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000893 Anti-Inflammatory Agents Substances that reduce or suppress INFLAMMATION. Anti-Inflammatory Agent,Antiinflammatory Agent,Agents, Anti-Inflammatory,Agents, Antiinflammatory,Anti-Inflammatories,Antiinflammatories,Antiinflammatory Agents,Agent, Anti-Inflammatory,Agent, Antiinflammatory,Agents, Anti Inflammatory,Anti Inflammatories,Anti Inflammatory Agent,Anti Inflammatory Agents

Related Publications

Srinivasa Rao Pedada, and Nagendra Sastry Yarla, and Pawan J Tambade, and Bhadrapura Lakkappa Dhananjaya, and Anupam Bishayee, and Kalle M Arunasree, and Gundala Harold Philip, and Gangappa Dharmapuri, and Gjumrach Aliev, and Swathi Putta, and Gururaja Rangaiah
Secretory phospholipase A2 inhibitors. Possible new anti-inflammatory agents.
January 1995, Agents and actions. Supplements,
Srinivasa Rao Pedada, and Nagendra Sastry Yarla, and Pawan J Tambade, and Bhadrapura Lakkappa Dhananjaya, and Anupam Bishayee, and Kalle M Arunasree, and Gundala Harold Philip, and Gangappa Dharmapuri, and Gjumrach Aliev, and Swathi Putta, and Gururaja Rangaiah
Synthesis and evaluation of tricyclic dipyrido diazepinone derivatives as inhibitors of secretory phospholipase A2 with anti-inflammatory activity.
January 2007, Current topics in medicinal chemistry,
Srinivasa Rao Pedada, and Nagendra Sastry Yarla, and Pawan J Tambade, and Bhadrapura Lakkappa Dhananjaya, and Anupam Bishayee, and Kalle M Arunasree, and Gundala Harold Philip, and Gangappa Dharmapuri, and Gjumrach Aliev, and Swathi Putta, and Gururaja Rangaiah
Indole-5-phenylcarbamate derivatives as human non-pancreatic secretory phospholipase A2 inhibitor.
October 2005, Bioorganic & medicinal chemistry letters,
Srinivasa Rao Pedada, and Nagendra Sastry Yarla, and Pawan J Tambade, and Bhadrapura Lakkappa Dhananjaya, and Anupam Bishayee, and Kalle M Arunasree, and Gundala Harold Philip, and Gangappa Dharmapuri, and Gjumrach Aliev, and Swathi Putta, and Gururaja Rangaiah
Phospholipase A2 inhibitors as potential anti-inflammatory agents.
January 2005, Current pharmaceutical design,
Srinivasa Rao Pedada, and Nagendra Sastry Yarla, and Pawan J Tambade, and Bhadrapura Lakkappa Dhananjaya, and Anupam Bishayee, and Kalle M Arunasree, and Gundala Harold Philip, and Gangappa Dharmapuri, and Gjumrach Aliev, and Swathi Putta, and Gururaja Rangaiah
Rhodanine Derivatives Containing 5-Aryloxypyrazole Moiety as Anti-inflammatory and Anticancer Agents.
February 2024, Chemistry & biodiversity,
Srinivasa Rao Pedada, and Nagendra Sastry Yarla, and Pawan J Tambade, and Bhadrapura Lakkappa Dhananjaya, and Anupam Bishayee, and Kalle M Arunasree, and Gundala Harold Philip, and Gangappa Dharmapuri, and Gjumrach Aliev, and Swathi Putta, and Gururaja Rangaiah
Coumarin Derivatives as Anti-inflammatory and Anticancer Agents.
January 2017, Anti-cancer agents in medicinal chemistry,
Srinivasa Rao Pedada, and Nagendra Sastry Yarla, and Pawan J Tambade, and Bhadrapura Lakkappa Dhananjaya, and Anupam Bishayee, and Kalle M Arunasree, and Gundala Harold Philip, and Gangappa Dharmapuri, and Gjumrach Aliev, and Swathi Putta, and Gururaja Rangaiah
Potential anticancer agents. I. Synthesis of isoxazole moiety containing quinazoline derivatives and preliminarily in vitro anticancer activity.
January 2015, Anti-cancer agents in medicinal chemistry,
Srinivasa Rao Pedada, and Nagendra Sastry Yarla, and Pawan J Tambade, and Bhadrapura Lakkappa Dhananjaya, and Anupam Bishayee, and Kalle M Arunasree, and Gundala Harold Philip, and Gangappa Dharmapuri, and Gjumrach Aliev, and Swathi Putta, and Gururaja Rangaiah
Design and synthesis of new indole containing biaryl derivatives as potent antiproliferative agents.
May 2021, Bioorganic chemistry,
Srinivasa Rao Pedada, and Nagendra Sastry Yarla, and Pawan J Tambade, and Bhadrapura Lakkappa Dhananjaya, and Anupam Bishayee, and Kalle M Arunasree, and Gundala Harold Philip, and Gangappa Dharmapuri, and Gjumrach Aliev, and Swathi Putta, and Gururaja Rangaiah
Synthesis and biological evaluation of new 3-substituted indole derivatives as potential anti-inflammatory and analgesic agents.
June 2007, Bioorganic & medicinal chemistry,
Srinivasa Rao Pedada, and Nagendra Sastry Yarla, and Pawan J Tambade, and Bhadrapura Lakkappa Dhananjaya, and Anupam Bishayee, and Kalle M Arunasree, and Gundala Harold Philip, and Gangappa Dharmapuri, and Gjumrach Aliev, and Swathi Putta, and Gururaja Rangaiah
Potent inhibitors of secretory phospholipase A2: synthesis and inhibitory activities of indolizine and indene derivatives.
September 1996, Journal of medicinal chemistry,
Copied contents to your clipboard!