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In order to identify potential calpain and cathepsin inhibitors we prepared 12 dihydroxychalcone analogues and tested their ability to inhibit μ-calpain, m-calpain, cathepsins B and L. In the calpain inhibition test, compound 10 exhibited the most active inhibitory activity against m-calpain with an IC50 value of 25.25±0.901μM. With respect to inhibition of cathepsins B and L, compound 13 exhibited the most potent inhibitory activity on cathepsin L and moderate inhibitory activity on cathepsin B with IC50 values of 2.80±0.100 and 11.47±0.087μM, respectively. Our results suggest the possibility of developing dual calpain and cathepsin inhibitors by properly modulating structures and/or combining the essential aspects of the functional group effective for specific calpain and cathepsin inhibition. ⓒ2013 Elsevier Inc. All rights reserved.
As a continuous study we prepared several alkylamine (n = 3-6) and evaluated for the pharmacological activity and mode of action. In the topoisomerase IIα (topo IIα) inhibition test, compound 4 showed strongest inhibitory activity among the compounds at 10 μM. Inhibitory activities of the compounds are in the order of 4 (n = 4) > 1 (n = 3) >> 5 (n = 5) □ 6 (n = 6); 8 (n = 4) >> 7 (n = 3) □ 9 (n = 5) □ 10 (n = 6) where n is the number of carbon in the aliphatic side chain in ring C and compounds 7-10 have additional methoxy group in ring A compared to compounds 1, 4-6. Compound 4 showed efficient cytotoxicities against T47D (IC: 0.93 ± 0.04 μM) and HCT15 (IC50: 0.78 ± 0.01 μM) cells, which are higher than etoposide. Compound 4 was also an ATP-competitive human topo IIα catalytic inhibitor with partially blocking human topo IIα-catalyzed ATP hydrolysis and intercalating into DNA. Compound 4 induced much less DNA damage than etoposide in HCT15 human colorectal carcinoma cells. Overall, compound 4 can be a potential anticancer agent acting as topo IIα catalytic inhibitor with low DNA damage.ⓒ2013 Elsevier Masson SAS. All rights reserved.
( Tara Man Kadayat ), ( Seojeong Park ), ( Kyu Yeon Jun ), ( Til Bahadur Thapa Magar ), ( Ganesh Bist ), ( Aarajana Shrestha ), ( Younghwa Na ), ( Youngjoo Kwon ), ( Eung Seok Lee ) 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
In continuation of our previous work, six hydroxylated 2,4-diphenyl-5H-indenoll ,2-b ]pyridine analogs were modified by introducing one chlorine functionality at ortho, meta or para position of the 2- or 4-phe-nyl ring. Eighteen new chlorinated compounds were thus prepared and assessed for topoisomerase inhi-bitory activity and cytotoxicity against HG15, T470, and HeLa cancer cell lines. All of the chlorinated compounds displayed significant cytotoxic effect, revealing potent anticancer activity against T470 breast cancer cells. This functional group modification allowed us to explore the importance of chlorine group substitution for the cytotoxic properties. The information reported here provides valuable insight for further study to develop new anticancer agents using related scaffolds.
( Pritam Thapa ), ( Tara Man Kadayat ), ( Seojeong Park ), ( Somin Shin ), ( Til Bahadur Thapa Magar ), ( Ganesh Bist ), ( Aarajana Shrestha ), ( Younghwa Na ), ( Youngjoo Kwon ), ( Eung Seok Lee ) 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
A new series of 2-phenol-4-chlorophenyl-6-aryl pyridines were designed, synthesized, and evaluated for topoisomerase (topo) I and II inhibitory activities as well as cytotoxic activity against four different human cancer cell lines such as HCT15, T47D, DU145, and Hela. Most of the tested compounds exhibited stronger topo II inhibitory activity at 100 μM as compared to etoposide. All the compounds, except 39, did not show topo I inhibitory activity. Interestingly, compounds that showed better topo II inhibition than etoposide have ortho- or para-chlorophenyl at 4-position of central pyridine, and none of the com-pounds possess meta-chlorophenyl. SAR study revealed the importance of ortha- or para-chlorophenyl at 4-position of the central pyridine for selective tapa II inhibitory activity. Similarly, all compounds possessing mere- or para-hydroxyphenyl moieties shawed moderate to significant cytotoxic effects. Particularly, compounds 27-37, and 39 which showed excellent cytotoxicity (IC<sub>50</sub> = 0.68-1.25 μM) against T47D breast cancer cells suggest the importance of meta- or para-hydroxyphenyl moiety at 2-position of the central pyridine for the design of anticancer agents with related scaffolds.
( Radha Karki ), ( Kyu Yeon Jun ), ( Tara Man Kadayat ), ( Somin Shin ), ( Til Bahadur Thapa Magar ), ( Ganesh Bist ), ( Aarajana Shrestha ), ( Younghwa Na ), ( Youngjoo Kwon ), ( Eung Seok Lee ) 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
As a continuous effort to develop novel antitumor agents, a new series of forty-five-2phenol-4-aryl-6-chlorophenyl pyridine compounds were synthesized and evaluated for cytotoxicity against four different human cancer cell lines(DU145, HCT15, T47D, and HeLa), and topoisomerase I and II inhibitory activity, Several compounds(10-15, 20, 22, 24, 28, 42, and 49) displayed strong to moderate dual topoisomerase I and II inhibitory activity at 100 μM. It was observed that hydroxyl and chlorine moiety at meta or para position of phenyl ring is favorable for dual topoisomerase inhibitory activity and cytotoxicity. Most of the compounds displayed stronger cytotoxicities than those of all positive controls against the HCT15 and T47D cell lines. For investigation of the structure-activity relationships, a 3D-QSAR analysis using the method of comparative molecular field analysis (CoMFA) was performed. The generated 3D contour maps can be used for further rational design of novel terpyridine derivatives as highly selective and potent cytotoxic agents.
Fluoroquinolones, represented by ciproxacin and norfloxacin, are well known clinical antimicrobial agents, and their phenyl ring expanded quinophenoxazines are reported as possible antitumor active compounds. These quinophenoxazines are known to inhibit DNA topoisomerase II essential for cell replication cycle. But there were no reports for topoisomerase I inhibition study for these compounds. In this report, we have prepared a few quinophenoxazine analogues and tested their topoisomerases I and II inhibitory activities and cytotoxicity. From the result, we found that qumophenoxazine analogues possessed strong topoisomerase I inhibitory capacity as well as topoisomerase II inhibition. Among the compounds prepared, A-62176 analogues showed strong topoisomerases I and II inhibitory activities. Interestingly, compound 8 missing the 3-aminopyrrolidine moiety at C2 position has similar potent inhibitory capacity against topoisomerases I & II at higher concentrations (20 and 10 uM, respectively). But compound 8 inhibited topoisomerase I function more selectively at lower concentration, 2 uM. Our observation mi&ht strongly implicate that fluoroquinophenoxazines can be developed as efficient topoisomerase I inhibitor with the elaborate modification.
In order to diversify the pharmacological activity of chalcones and extend the scaffold of topoisomerase and cathepsins B and L inhibitors, we have designed and synthesized total 18 chalcone compounds and tested their biological activity. In the topoisomerase inhibition test, most analogues in group III and IV except compound 11 exhibited more efficient topoisomerase I inhibitory activity than camptothecin at 20 μM. Compounds 15, 16 and 18 in group IV showed significant cathepsin B and L inhibitory activity. Among the compounds, compound 15 was most active with IC50 values of 1.81±0.05 μM oncathepsin B and 3.15±0.07 μM on cathepsin L, respectively. Compound 15 also showed most potent cytotoxic activity against T47D and SNU638 cells with IC50 values of 1.37±0.05 μM and 0.62±0.01 μM, respectively. Overall, although more compounds should be tested and analyzed for clear SAR againsttopoisomerase I and cathepsin B and L, compound 15 showed consistent inhibitory ability on the tested assays, which can implicate the cytotoxic activity of compound 15 on topoisomerase I andcathepsin B and L inhibitory pathways. ⓒ2013 Elsevier Ltd. All rights reserved.
우미희(Mi Hee Woo), 이응석(Eung-Seok Lee), 최란(Lan Choi), 손경희(Kyung-Hee Sohn), 김인규(In-Kyu Kim), 황보경(Kyoung Hwangbo), 이은영(Eunyoung Lee), 손종근(Jong-Keun Son), 나영화(Younghwa Na), 장인혜(Inhye Chang) 大韓藥學會 2002 大韓藥學會 總會 및 學術大會 Vol.2002 No.2
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As an effort to find a new scaffold for α-glucosidase inhibition, we have prepared total 11 phenylalkylated piperazine derivatives and tested their α-glucosidase inhibitory activities. Compounds 8 (IC50=2.73±0.075 mM) possessing two 3-methoxyphenethyl group on 1,4-position of piperazine showed comparable potency to acarbose used as reference. But other compounds were inactive to α-glucosidase. The result indicated that proper substituents on the piperazine can engender α-glucosidase inhibitory activities on the piperazine derivatives.
( Pritam Thapa ), ( Kyu Yeon Jun ), ( Tara Man Kadayat ), ( Chanmi Park ), ( Zhi Zheng ), ( Til Bahadur Thapa Magar ), ( Ganesh Bist ), ( Aarajana Shrestha ), ( Younghwa Na ), ( Youngjoo Kwon ), ( Eung Seok Lee) 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
To develop novel selective topoisomerase II inhibitors, we designed and synthesized a series of conforma-tionally constrained hydroxylated 4-phenyl-2-aryl chromenopyridines and evaluated their to poi so-merase inhibitory activity and cytotoxicity against three human cancer cell lines (DU145, HCn5, and T47D) and a normal cell line (MCF10A). All of the prepared compounds displayed stronger or similar topoisomerase II inhibitory activity as well as cytotoxicity against three human cancer cell lines com-pared to etoposide. Compounds 10., 109, 11., 11f, 11g, 12., 12f, and 12g especially showed stronger topoisornerase II inhibitory activity as compared to etoposide at both 100 μM and 20 μM. A structure-ac-tivity relationship study revealed that hydroxyphenyl moiety at 4-position of pyridine and ortho-hydrox-yphenyl or thienyl moiety at 2-position of pyridine has an important role in displaying selective topoisomerase II inhibition. The compound 12b with para-hydroxyphenyl and meta-hydroxyphenyl at 4- and 2-position of pyridine. respectively, showed the most significant cytotoxicity against all three can-cer cell lines, whereas less cytotoxicity to a normal cell line as compared to adriamycin.