Novel, selective acrylamide linked quinazolines for the treatment of double mutant EGFR-L858R/T790M Non-Small-Cell lung cancer (NSCLC).
Autor: | Pawara R; Division of Computer-Aided Drug Design, Dept. of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, District, Dhule 425 405, Maharashtra, India., Ahmad I; Division of Computer-Aided Drug Design, Dept. of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, District, Dhule 425 405, Maharashtra, India., Nayak D; Cancer Biology Division, KIIT School of Biotechnology, Kalinga Institute of Industrial Technology, Campus-11, Patia, Bhubaneswar 751024, Odisha, India., Wagh S; Division of Computer-Aided Drug Design, Dept. of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, District, Dhule 425 405, Maharashtra, India., Wadkar A; Division of Computer-Aided Drug Design, Dept. of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, District, Dhule 425 405, Maharashtra, India., Ansari A; Department of Pharmaceutical Chemistry, Shri Vile Parle Kelavani Mandal's Institute of Pharmacy, Dhule 424001, Maharashtra, India., Belamkar S; Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKMs NMIMS V. L. Mehta Road Vile Parle (W) Mumbai, 400056, Maharashtra, India., Surana S; Division of Computer-Aided Drug Design, Dept. of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, District, Dhule 425 405, Maharashtra, India., Nath Kundu C; Cancer Biology Division, KIIT School of Biotechnology, Kalinga Institute of Industrial Technology, Campus-11, Patia, Bhubaneswar 751024, Odisha, India., Patil C; Department of Pharmacology, Delhi Pharmaceutical Sciences and Research University, New Delhi 110017, India., Patel H; Division of Computer-Aided Drug Design, Dept. of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, District, Dhule 425 405, Maharashtra, India. Electronic address: hpatel_38@yahoo.com. |
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Jazyk: | angličtina |
Zdroj: | Bioorganic chemistry [Bioorg Chem] 2021 Oct; Vol. 115, pp. 105234. Date of Electronic Publication: 2021 Aug 08. |
DOI: | 10.1016/j.bioorg.2021.105234 |
Abstrakt: | T790M mutation is the most common mechanism of acquired resistance to first-generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs). To overcome this resistance, 4-anilinoquinazoline-based irreversible inhibitors afatinib, dacomitinib has been developed. However, the clinical application of these irreversible inhibitors is limited due to its narrow selectivity against L858R/T790M mutant EGFR. In an attempt to develop potent and selective EGFR T790M inhibitors, we have designed and synthesized two series of novel acrylamide linked quinazolines. Among them, compounds 2i (IC (Copyright © 2021 Elsevier Inc. All rights reserved.) |
Databáze: | MEDLINE |
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