دورية أكاديمية

Synthesis, biological evaluation, and molecular docking of novel 1,3,4-substituted-thiadiazole derivatives as potential anticancer agent.

التفاصيل البيبلوغرافية
العنوان: Synthesis, biological evaluation, and molecular docking of novel 1,3,4-substituted-thiadiazole derivatives as potential anticancer agent.
المؤلفون: Shaikh SA; Department of Chemistry, Savitribai Phule Pune University, Kr. V. N. Naik Shikshan Prasarak Sanstha's Arts, Commerce and Science College, Canada Corner, Nashik, Maharashtra, 422002, India. saminshaikh80@gmail.com.; Department of Chemistry, Savitribai Phule Pune University, KTHM College, Nashik, Maharashtra, 422002, India. saminshaikh80@gmail.com., Wakchaure SN; Department of Synthetic R & D, Delta Finochem Pvt. Ltd., G. No. 350, Wadivarhe, Igatpuri, Nashik, Maharashtra, 422403, India. satish_nclpune@yahoo.co.in.; Friedrich Alexander University Erlangen-Nuremberg (FAU), 91058, Erlangen, Germany. satish_nclpune@yahoo.co.in., Labhade SR; Department of Chemistry, Savitribai Phule Pune University, KTHM College, Nashik, Maharashtra, 422002, India., Kale RR; Department of Chemistry, Savitribai Phule Pune University, KTHM College, Nashik, Maharashtra, 422002, India., Alavala RR; SVKM's NMIMS, Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, Vile Parle (W), Mumbai, Maharashtra, 400056, India., Chobe SS; Department of Chemistry, Savitribai Phule Pune University, M.G.Vs. L. V. H. Arts, Science and Commerce College, Panchavati, Nashik, Maharashtra, 422003, India., Jain KS; Department of Chemistry, Savitribai Phule Pune University, Kr. V. N. Naik Shikshan Prasarak Sanstha's Arts, Commerce and Science College, Canada Corner, Nashik, Maharashtra, 422002, India., Labhade HS; Department of Chemistry, Savitribai Phule Pune University, KTHM College, Nashik, Maharashtra, 422002, India., Bhanushali DD; Department of Chemistry, Savitribai Phule Pune University, Kr. V. N. Naik Shikshan Prasarak Sanstha's Arts, Commerce and Science College, Canada Corner, Nashik, Maharashtra, 422002, India.
المصدر: BMC chemistry [BMC Chem] 2024 Jun 27; Vol. 18 (1), pp. 119. Date of Electronic Publication: 2024 Jun 27.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Springer Nature Country of Publication: Switzerland NLM ID: 101741142 Publication Model: Electronic Cited Medium: Internet ISSN: 2661-801X (Electronic) Linking ISSN: 2661801X NLM ISO Abbreviation: BMC Chem Subsets: PubMed not MEDLINE
أسماء مطبوعة: Original Publication: Cham, Switzerland : Springer Nature, [2019]-
مستخلص: In an attempt to develop potent anti-cancer agents, a new 1,3,4-substituted-thiadiazole derivatives (8b-g), starting from 4-substituted-thiazol-2-chloroacetamides (4b-g), were synthesized and evaluated for their cytotoxic effects on multiple human cancer cell lines, including the hepatocellular carcinoma (HEPG-2), human lung carcinoma (A549), human breast carcinoma (MCF-7) and pseudo-normal human embryonic liver (L02) cancer cell lines by an MTT assay. Among all synthesized compounds, compound 8d showed the potent anti-cancer activities with GI 50 values of 2.98, 2.85 and 2.53 μM against MCF-7, A549 and HepG-2 cell lines respectively as compared to standard drug Doxorubicin. Furthermore, molecular modelling studies have spotlighted the anchoring role of 1,3,4-substituted-thiadiazole moiety in bonding and hydrophobic interaction with the key amino acid residues. Therefore, these results can provide promising starting points for further development of best anti-cancer agents.
(© 2024. The Author(s).)
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فهرسة مساهمة: Keywords: Anticancer agents; Antiproliferative activity; Molecular docking; Synthesis optimization; Thiazole-Thiadiazole compounds
تواريخ الأحداث: Date Created: 20240627 Latest Revision: 20240629
رمز التحديث: 20240629
مُعرف محوري في PubMed: PMC11210122
DOI: 10.1186/s13065-024-01196-1
PMID: 38937800
قاعدة البيانات: MEDLINE
الوصف
تدمد:2661-801X
DOI:10.1186/s13065-024-01196-1