Synthesis, cytotoxic, and carbonic anhydrase inhibitory effects of new 2-(3-(4-methoxyphenyl)-5-(aryl)-4,5-dihydro-1H-pyrazol-1-yl)benzo[d]thiazole derivatives
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作者:
Tugrak, Mehtap
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Ataturk Univ, Fac Pharm, Dept Pharmaceut Chem, Erzurum, TurkeyAtaturk Univ, Fac Pharm, Dept Pharmaceut Chem, Erzurum, Turkey
Tugrak, Mehtap
[1
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Gul, Halise Inci
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Ataturk Univ, Fac Pharm, Dept Pharmaceut Chem, Erzurum, TurkeyAtaturk Univ, Fac Pharm, Dept Pharmaceut Chem, Erzurum, Turkey
Gul, Halise Inci
[1
]
Sakagami, Hiroshi
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Meikai Univ, Div Pharmacol, Res Inst Odontol, Sakado, Saitama, JapanAtaturk Univ, Fac Pharm, Dept Pharmaceut Chem, Erzurum, Turkey
Sakagami, Hiroshi
[2
]
Gulcin, Ilhami
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Ataturk Univ, Fac Sci, Dept Chem, Erzurum, TurkeyAtaturk Univ, Fac Pharm, Dept Pharmaceut Chem, Erzurum, Turkey
Gulcin, Ilhami
[3
]
机构:
[1] Ataturk Univ, Fac Pharm, Dept Pharmaceut Chem, Erzurum, Turkey
[2] Meikai Univ, Div Pharmacol, Res Inst Odontol, Sakado, Saitama, Japan
[3] Ataturk Univ, Fac Sci, Dept Chem, Erzurum, Turkey
2-(3-[4-Methoxyphenyl]-5-aryl-4,5-dihydro-1H-pyrazol-1-yl)benzo[d]thiazoles (1b-7b) were synthesized for the first time except 1b, and spectral methods such as H-1 NMR, C-13 NMR and HRMS were utilized to illuminate the chemical structures of the synthesized compounds. Phenyl (1b), 2-methoxyphenyl (2b), 4-methoxyphenyl (3b), 4-methoxy-3-hydroxyphenyl (4b), 2,5-dimethoxyphenyl (5b), 3,4,5-trimethoxyphenyl (6b), or thiophene-2-yl (7b) was used as a aryl part. The inhibitory effects of the compounds were evaluated toward human carbonic anhydrase I and II enzymes (hCA I and hCA II). In vitro cytotoxic effects of the compounds against human oral squamous carcinomas and human normal oral cells were carried out via MTT. The compounds (1b-7b) had Ki values of 36.87 +/- 11.62-66.24 +/- 2.99 mu M (hCA I) and 22.66 +/- 1.41-89.95 +/- 6.25 mu M (hCA II). Compounds 1b (Ki = 36.87 +/- 11.62 mu M) toward hCA I, 6b (Ki = 22.66 +/- 1.41 mu M) toward hCA II had significant enzyme inhibitory potency. Compound 6b had the highest tumor selectivity (TS = 29.3) and potency selectivity expression (PSE = 272.3) values. Therefore, compounds 1b and 6b with CAs inhibition effect and compound 6b with the cytotoxicity may be forwarded to further studies as potent compounds.
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Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
Aboul-Enein, Mohamed N.
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El-Azzouny, Aida A.
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Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
El-Azzouny, Aida A.
;
Attia, Mohamed I.
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Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi ArabiaNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
Attia, Mohamed I.
;
Maklad, Yousreya A.
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Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Pharmacol Grp, Giza 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
Maklad, Yousreya A.
;
Amin, Kamilia M.
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Cairo Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
Amin, Kamilia M.
;
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Abdel-Rehim, Mohamed
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El-Behairy, Mohammed F.
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Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
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Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
Aboul-Enein, Mohamed N.
;
El-Azzouny, Aida A.
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Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
El-Azzouny, Aida A.
;
Attia, Mohamed I.
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Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi ArabiaNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
Attia, Mohamed I.
;
Maklad, Yousreya A.
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Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Pharmacol Grp, Giza 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
Maklad, Yousreya A.
;
Amin, Kamilia M.
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Cairo Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt
Amin, Kamilia M.
;
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Abdel-Rehim, Mohamed
;
El-Behairy, Mohammed F.
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Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, EgyptNatl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt