Research

Chemical Sciences

Title :

A Convergent Synthetic Platform to Access Marine Natural Products, Conoidecyclics A, B, and C

Area of research :

Chemical Sciences

Principal Investigator :

Dr. Thirupathi Barla, Indian Institute of Science Education and Research (IISER) Berhampur, Odisha

Timeline Start Year :

2022

Timeline End Year :

2025

Contact info :

Equipments :

Details

Executive Summary :

A number of marine derived natural products have recently been transformed into clinically approved drugs, such as Omega-3-acid ethyl esters, Eicosapentaenoic acid ethyl ester, Cytarabine, Vidarabine, Nelarabine, Ziconotide, Plitidepsin, Trabectedin, Lurbinectedin, Eribulin mesylate, Brentuximab vedotin, Enfortumab vedotin, Polatuzumab vedotin, Belantamab mafodotin. Additionally, 30 of such marine natural products are in various phases of clinical trials. Therefore, total syntheses of such marine-derived natural products or their analogues are exhilarating research area. Recently, Chakraborthy and Dhara isolated novel macrolides, conoidecyclics A-C from marine macroalga Turbinaria conoides from coastal zones of the Indian subcontinent. Conoidecyclics A showed higher attenuation potential against 5-lipoxygenase than an anti-inflammatory agent, ibuprofen, it exhibited potential inhibitory activity against pro-inflammatory enzyme with higher selectivity index than anti-inflammatory agent ibuprofen. In addition, conoidecyclics A could effectively attenuate and act as a negative regulator of insulin signaling thereby acting as a selective bioactive potential to regulate multiple mechanisms implicated in the pathogenesis of inflammation, hypertension, and type-2 diabetes. Apart from the above-mentioned activities, conoidecyclics A showed drug-likeness properties and impressive pharmacokinetic parameters as acceptable for oral bioavailability. Considering these potent biological properties and interesting structural features, our objective is to develop a novel synthetic platform to achieve a new class of natural products, conoidecyclics A, B, and C. PI is hoping that the development of a synthetic route to access those natural products may certainly help to find out their complete biological profile, it may also help us to find a lead compound(s) for drug discovery and development. Therefore, the development of a synthetic strategy to obtain these natural products is an important area of research as it allows the development of new strategies and new chemistry that would play important role in organic synthesis.

Total Budget (INR):

40,44,832

Organizations involved