40176-01-0Relevant articles and documents
A class of carbonic anhydrase IX/XII–selective carboxylate inhibitors
Alhameed, Rakia Abd,Almarhoon, Zainab,Berrino, Emanuela,El-Faham, Ayman,Supuran, Claudiu T.
, p. 549 - 554 (2020)
A small series of 2,4-dioxothiazolidinyl acetic acids was prepared from thiourea, chloroacetic acid, aromatic aldehydes, and ethyl-2-bromoacetate. They were assayed for the inhibition of four physiologically relevant carbonic anhydrase (CA, EC 4.2.1.1) isoforms of human (h) origin, the cytosolic hCA I and II, and the transmembrane hCA IX and XII, involved among others in tumorigenesis (hCA IX and XII) and glaucoma (hCA II and XII). The two cytosolic isoforms were not inhibited by these carboxylates, which were also rather ineffective as hCA IX inhibitors. On the other hand, they showed submicromolar hCA XII inhibition, with KIs in the range of 0.30–0.93 μM, making them highly CA XII-selective inhibitors.
Synthesis and antimicrobial activity of a new series of thiazolidine-2,4-diones carboxamide and amino acid derivatives
Alhameed, Rakia Abd,Almarhoon, Zainab,Bukhari, Sarah I.,El-Faham, Ayman,De La Torre, Beatriz G.,Albericio, Fernando
, (2020/01/13)
Novel thiazolidine-2,4-dione carboxamide and amino acid derivatives were synthesized in excellent yield using OxymaPure/N,N'-diisopropylcarbodimide coupling methodology and were characterized by chromatographic and spectrometric methods, and elemental ana
Design, synthesis, molecular docking and anticancer evaluations of 5-benzylidenethiazolidine-2,4-dione derivatives targeting VEGFR-2 enzyme
Eissa, Ibrahim H.,El-Adl, Khaled,El-Hddad, Sanadelaslam S. A.,El-Helby, Abdel-Ghany A.,M. I. A. Shoman, Fatma,Sakr, Helmy
, (2020/07/13)
Novel series of 5-benzylidenethiazolidine-2,4-dione derivatives 4a-c-8a-f were designed, synthesized and evaluated for anticancer activity against HepG2, HCT-116 and MCF-7 cell lines. MCF-7 was the most sensitive cell line to the influence of the new derivatives. In particular, compound 8f was found to be the most potent derivative overall the tested compounds against the three HepG2, HCT116 and MCF-7 cancer cell lines with IC50 = 11.19 ± 0.8, 8.99 ± 0.7 and 7.10 ± 0.4 μM respectively. Compound 8f exhibited lower activity than sorafenib, (IC50 = 9.18 ± 0.6, 8.37 ± 0.7 and 5.10 ± 0.4 μM respectively), against HepG2 and HCT116 but exhibited nearly the same activity against MCF-7 cancer cell lines respectively. Also, this compound displayed lower activity than doxorubicin, (IC50 = 7.94 ± 0.6, 8.07 ± 0.8 and 6.75 ± 0.4 μM respectively), against HepG2 and HCT116 but nearly the same activity against MCF-7cell lines respectively. The most active derivatives 6c,d,f,g and 8a-f were evaluated for their inhibitory activities against VEGFR-2. The elongation of the structures to have distal moieties enhanced anticancer and VEGFR-2 inhibitory activities as in compounds 8a-f. Among them, compounds 8f was found to be the most potent derivative that inhibited VEGFR-2 at IC50 value of 0.22 ± 0.02 μM, which is nearly the half as that of sorafenib IC50 value (0.10 ± 0.02 μM). Furthermore, molecular design was performed to investigate their binding mode and affinities towards VEGFR-2 receptor. The data obtained from docking studies were highly correlated with that obtained from the biological screening.
