Takamatsu, Kayo; Takano, Atsushi; Yakushiji, Nobumasa; Morishita, Ken-ichi; Matsuura, Nobuyasu; Makishima, Makoto; Ali, Hamed Ismail; Akaho, Eiichi; Tai, Akihiro; Sasaki, Kenji; Kakuta, Hiroki published the artcile< Reduction of lipophilicity at the lipophilic domain of RXR agonists enables production of subtype preference: RXRα-preferential agonist possessing a sulfonamide moiety>, Formula: C7H7ClN2O2, the main research area is sulfonamide derivative preparation structure RXR agonist lipophilicity antitumor.
Retinoid X receptor agonists (RXR agonists, rexinoids) are interesting candidates for the treatment of cancers such as tamoxifen-resistant breast cancer and taxol-resistant lung cancer. However, well-known RXR agonists possess a strong lipophilic character. In addition, although RXR has three subtypes, no subtype-selective RXR agonists are known. Thus the authors aimed to produce less-lipophilic and subtype-selective RXR agonists. By designing sulfonamide-type RXR agonists, compound (I) was found to prefer RXRα over RXRβ and RXRγ, although the potency is less than the potencies of well-known RXR pan-agonists. Moreover, the results suggest that the reduction of lipophilicity at the hydrophobic interaction region of RXR agonists enables production of RXR subtype preference. The finding will be useful for the creation of more potent and less-lipophilic subtype-selective RXR agonists aimed at the reduction of undesirable side effects.
ChemMedChem published new progress about Homo sapiens. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Formula: C7H7ClN2O2.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia