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. 2022 Jun 21;27(13):3994. doi: 10.3390/molecules27133994

Table 1.

Thiazole-ring-bearing drug candidates under intensive preclinical/clinical investigations.

Bioactive Compounds Remarks/Conclusions
graphic file with name molecules-27-03994-i001.jpg Fatostatin (125B11): A specific inhibitor of sterol response element-binding proteins (SREBPs) is a newly customized thiazole analogue combined with two aryl groups. Fatostatin inhibits proliferation and increases cellular deaths in cancer cells. The drug may possibly be prescribed in the therapy of uterine carcinoma [44].
graphic file with name molecules-27-03994-i002.jpg Mirabegron (YM 178): The medication is a selective β3-adrenoceptor stimulant that was recently licensed to alleviate overactive bladder (OAB) [45].
graphic file with name molecules-27-03994-i003.jpg Ziritaxestat (GLPG1690): An autotaxin inhibitor is being optimized as a potential therapeutic candidate. The medication is still in development because phase 2 clinical studies for the clinical use of Systemic Sclerosis were unsuccessful [46,47].
graphic file with name molecules-27-03994-i004.jpg WEHI-539 HCl (WEHI-539 hydrochloride): The therapeutic candidate binds to BCL-XL with great affinity and specificity, killing cells effectively by inhibiting its pro-survival function. The molecule is in the developmental stage and is currently being optimized to achieve better physicochemical parameters. If further developed, the medicine could be approved for the management of a host of drug-resistant tumors [48].
graphic file with name molecules-27-03994-i005.jpg O4I2: The drug candidate is a powerful Oct3/4 inducer that possibly be prescribed to make iPSCs. This molecule is in a preclinical developmental stage and may possibly be used in the treatment of a variety of cancer [49].
graphic file with name molecules-27-03994-i006.jpg TP0427736: The compound is an effective inhibitor of ALK5 kinase activity. It also suppresses TGF-β1-induced phosphorylation of Smad2/3 in A549 cells. The drug is being optimized for its potential use in androgenic alopecia [50].
graphic file with name molecules-27-03994-i007.jpg SRT2104 (GSK2245840): The compound is a selective Sirtuin 1(SIRT1) activator engaged in energy homeostasis management. The drug candidate is being investigated for clinical use for Atrophy, Sepsis, Psoriasis, Type 2 Diabetes Mellitus, and Muscular Dystrophy [51,52].
graphic file with name molecules-27-03994-i008.jpg IRAK inhibitor 6: The therapeutic candidate is a selective Renal Carcinoma Antigen NY REN 64 blocker that can possibly be used to manage bone degradation and rheumatoid arthritis-induced joint inflammation [53].
graphic file with name molecules-27-03994-i009.jpg SC75741: The therapeutic candidate is a highly effective NF-B inhibitor. Due to its efficacy at inhibiting influenza virus replication, SC75741 is being developed to treat avian influenza-A virus infections [54].
graphic file with name molecules-27-03994-i010.jpg SRT3025: The active agent is a small molecule activator of the SIRT1 enzyme. The therapy could be used to manage Fanconi anaemia [55].
graphic file with name molecules-27-03994-i011.jpg UM-164: The active substance is a highly powerful dual c-Src/p38 inhibitor that inhibits both p38 and p38 and has a binding constant Kd of 2.7 nM for c-Src. The drug is the subject of a great deal of research since it claims to be able to cure triple-negative breast cancer [56].