{"id":566,"date":"2026-08-11T19:52:34","date_gmt":"2026-08-11T19:52:34","guid":{"rendered":"https:\/\/syrian-biomedica.com\/bayan-zoatier\/"},"modified":"2026-08-15T09:00:40","modified_gmt":"2026-08-15T09:00:40","slug":"bayan-zoatier","status":"publish","type":"page","link":"https:\/\/syrian-biomedica.com\/ar\/bayan-zoatier\/","title":{"rendered":"Bayan Zoatier"},"content":{"rendered":"

Bayan Zoatier<\/strong><\/h1>\n

Bayan Zoatier\u00b9, K. Gizem Yildiztekin\u00b2, M. Abdullah Alagoz\u00b3, Ceylan Hepokur\u2074, Serdar Burmaoglu\u2075, Oztekin Algul\u00b9\u02d2\u2076<\/p>\n

\u00b9 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin, T\u00fcrkiye
\u00b2 Department of Toxicology, Faculty of Pharmacy, Erzincan Binali Y\u0131ld\u0131r\u0131m University, Erzincan, T\u00fcrkiye \u00b3 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Inonu University, Malatya, T\u00fcrkiye
\u2074 Department of Biochemistry, Faculty of Pharmacy, Sivas Cumhuriyet University, Sivas, T\u00fcrkiye
\u2075 Department of Chemistry, Faculty of Science, Atat\u00fcrk University, Erzurum, T\u00fcrkiye
\u2076 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Erzincan Binali Y\u0131ld\u0131r\u0131m University, Erzincan, T\u00fcrkiye<\/h1>\n

\n

Development of Potent Type V MAPK Inhibitors: Design, Synthesis, and Biological Evaluation of Benzothiazole Derivatives Targeting p38\u03b1 MAPK in Breast Cancer Cells<\/strong><\/p>\n<\/div>\n

\n

Background<\/u>:<\/strong><\/p>\n

The p38\u03b1 mitogen-activated protein kinase (p38\u03b1 MAPK) pathway plays an important role in regulating cellular processes involved in cancer development and progression. Type V MAPK inhibitors represent a promising strategy because they can interact with both the ATP-binding site and an additional allosteric lipid-binding region, potentially improving target selectivity.<\/p>\n<\/p>\n

Objectives<\/u>:<\/strong><\/p>\n

This study aimed to design, synthesize, and evaluate benzothiazole derivatives as potential Type V p38\u03b1 MAPK-targeting compounds with antiproliferative activity against breast cancer cells.<\/p>\n<\/p>\n

Methods<\/u>:<\/strong><\/p>\n

A series of 28 benzothiazole derivatives was synthesized and evaluated for antiproliferative activity against estrogen receptor-positive MCF-7 and estrogen receptor-negative MDA-MB-231 breast cancer cells, together with normal L929 fibroblast cells, using the MTT assay. The most active compounds were further investigated for their effects on p38\u03b1 MAPK levels. Molecular docking and 100 ns molecular dynamics simulations were performed to analyze binding interactions and stability within the p38\u03b1 MAPK binding regions.<\/p>\n<\/p>\n

Results<\/u>:<\/strong><\/p>\n

Several benzothiazole derivatives demonstrated promising antiproliferative activity. Compounds 15 and 19 showed the strongest activity against MCF-7 cells, with IC\u2085\u2080 values of 8.83 \u00b1 0.43 and 6.19 \u00b1 1.05 \u03bcM, respectively. Compound 19 exhibited favorable selectivity indices against MCF-7 (SI = 15.17) and MDA-MB-231 (SI = 8.74) cells. Compounds 19 and 15 showed reduced p38\u03b1 MAPK levels of 0.112 and 0.155 ng\/\u03bcg protein, respectively. Molecular docking revealed favorable interactions of these compounds within both ATP-binding and lipid-binding regions of p38\u03b1 MAPK, while molecular dynamics simulations demonstrated stable protein\u2013ligand interactions throughout the 100 ns simulation period.<\/p>\n<\/p>\n

Conclusion<\/u>:<\/strong><\/p>\n

This study identified benzothiazole derivatives as promising p38\u03b1 MAPK-targeting compounds with antiproliferative activity against breast cancer cells. The integration of biological evaluation and computational analysis supports further optimization of these compounds as potential anticancer lead structures.<\/p>\n<\/p>\n

Keywords<\/u>:<\/strong><\/p>\n

Benzothiazole derivatives; p38\u03b1 MAPK; Antiproliferative activity; Breast cancer; Molecular docking<\/p>\n<\/div>\n


\n<\/p>\n","protected":false},"excerpt":{"rendered":"

Bayan Zoatier Bayan Zoatier\u00b9, K. Gizem Yildiztekin\u00b2, M. Abdullah Alagoz\u00b3, Ceylan Hepokur\u2074, Serdar Burmaoglu\u2075, Oztekin Algul\u00b9\u02d2\u2076 \u00b9 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin, T\u00fcrkiye \u00b2 Department of Toxicology, Faculty of Pharmacy, Erzincan Binali Y\u0131ld\u0131r\u0131m University, Erzincan, T\u00fcrkiye \u00b3 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Inonu University, Malatya, T\u00fcrkiye \u2074 Department […]<\/p>\n","protected":false},"author":1,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"footnotes":"","_et_pb_custom_css":""},"class_list":["post-566","page","type-page","status-publish","hentry"],"_et_pb_custom_css":"","_links":{"self":[{"href":"https:\/\/syrian-biomedica.com\/ar\/wp-json\/wp\/v2\/pages\/566","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/syrian-biomedica.com\/ar\/wp-json\/wp\/v2\/pages"}],"about":[{"href":"https:\/\/syrian-biomedica.com\/ar\/wp-json\/wp\/v2\/types\/page"}],"author":[{"embeddable":true,"href":"https:\/\/syrian-biomedica.com\/ar\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/syrian-biomedica.com\/ar\/wp-json\/wp\/v2\/comments?post=566"}],"version-history":[{"count":3,"href":"https:\/\/syrian-biomedica.com\/ar\/wp-json\/wp\/v2\/pages\/566\/revisions"}],"predecessor-version":[{"id":599,"href":"https:\/\/syrian-biomedica.com\/ar\/wp-json\/wp\/v2\/pages\/566\/revisions\/599"}],"wp:attachment":[{"href":"https:\/\/syrian-biomedica.com\/ar\/wp-json\/wp\/v2\/media?parent=566"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}