<?xml version="1.0" encoding="UTF-8"?><xml><records><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Sathe, Balaji Dashrath</style></author><author><style face="normal" font="default" size="100%">Meenakshi, Meenakshi</style></author><author><style face="normal" font="default" size="100%">Murti, Yogesh</style></author><author><style face="normal" font="default" size="100%">Mane, Madhav Shivaji</style></author><author><style face="normal" font="default" size="100%">Pandey, Sarvesh Kumar</style></author><author><style face="normal" font="default" size="100%">Mahajan, Shriya</style></author><author><style face="normal" font="default" size="100%">Rawat, Pramod</style></author><author><style face="normal" font="default" size="100%">Kandhari, Harsimrat</style></author><author><style face="normal" font="default" size="100%">Goel, Kapil Kumar</style></author><author><style face="normal" font="default" size="100%">Dwivedi, Ashish Ranjan</style></author><author><style face="normal" font="default" size="100%">Rathod, S. V.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Development of new N -4-[(7-Chloro-5-methylpyrrolo[2,1-f ] [1,2,4]triazin-4-yl)oxy]-3-fluorophenylbenzenesulfonamide analogues: exploring anticancer potential through MerTK inhibition</style></title><secondary-title><style face="normal" font="default" size="100%">Synlett</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">cancer chemotherapeutics</style></keyword><keyword><style  face="normal" font="default" size="100%">kinase inhibitors</style></keyword><keyword><style  face="normal" font="default" size="100%">metabolic studies</style></keyword><keyword><style  face="normal" font="default" size="100%">pyrrolotriazines</style></keyword><keyword><style  face="normal" font="default" size="100%">sulfonamides</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2025</style></year><pub-dates><date><style  face="normal" font="default" size="100%">MAR</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">36</style></volume><pages><style face="normal" font="default" size="100%">522-530</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;
	Mer proto-oncogene tyrosine-protein kinase (MerTK), a part of the TAM (TYRO3, AXL, and MerTK) family, is directly correlated with metastasis and various types of cancers. The inhibition of this receptor is a promising strategy for more-effective chemotherapy. Considering the pharmacophoric features of the active domain of MerTK and the structural characteristics of the investigational drug BMS794833, we designed five new N -{4-[(7-chloro-5-methylpyrrolo[2,1- f ][1,2,4]triazin-4-yl)oxy]-3-fluorophenyl}benzenesulfonamide analogues. In cytotoxicity studies, one of the analogues displayed a significantly higher cytotoxicity than cisplatin. It showed IC50 values of 2.09, 1.96, and 3.08 mu M against A549, MCF-7, and MDA-MB-231 cancer cell lines, respectively. In drug metabolism and pharmacokinetic studies, it was the most stable analogue and displayed a moderate MerTK inhibitory potential. Molecular-docking studies were performed to corroborate the MerTK inhibition, and the same analogue achieved the most significant docking score (-12.33 kcal/mol). Docking interactions demonstrated that the imine and amine group of the 3-chloropyridine moiety of BMS794833 formed hydrogen bonds with the main chain of the ATP pocket residue Met674, while the oxygen atoms of the 4-oxo-1,4-dihydropyridine-3-carboxamide moiety established hydrogen bonds with the Lys619 and Asp741 amino acid residues of the allosteric pocket of MerTK protein. These promising results provide evidence that the N -{4-[(7-chloro-5-methylpyrrolo[2,1- f ][1,2,4]triazin-4-yl)oxy]-3-fluorophenyl}benzenesulfonamide pharmacophore can give potential insights into the development of new MerTK inhibitors.&lt;/p&gt;
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