Novel Pyrazolo[3,4-b]pyridine Derivatives : Synthesis, Characterization, Antimicrobial and Antiproliferative Profile
-
- Salem Marwa Sayed
- Synthetic Organic Chemistry Laboratory, Department of Chemistry, Faculty of Science, Ain Shams University
-
- Ali Mohamed Ahmed Mohamed
- Department of Biochemistry, Faculty of Science, Ain Shams University
書誌事項
- タイトル別名
-
- Novel Pyrazolo[3,4-<i>b</i>]pyridine Derivatives: Synthesis, Characterization, Antimicrobial and Antiproliferative Profile
この論文をさがす
説明
Three novel series of pyridine derivatives, namely Schiff’s bases, 4-thiazolidinones and azetidin-2-ones bearing pyrazolo[3,4-b]pyridine moiety, have been synthesized. The chemical structures of the synthesized compounds were characterized. The compounds were tested for their antimicrobial activity using the agar well diffusion and broth macrodilution methods. The compounds were also evaluated for their antiproliferative activity using the sulforhodamine B (SRB) assay. The majority of the tested compounds exhibited slight to high antimicrobial activity against the test microorganisms with minimum inhibitory concentrations (MICs) of 0.12–62.5 µg/mL when compared to that of 3 standard antimicrobial agents (Ampicillin, 0.007–0.03 µg/mL; Gentamicin; 0.015–0.24 µg/mL; and Amphotericin B, 0.03–0.98 µg/mL). Compound (7b) was found to be nearly as active as the standard antimicrobial drug Amphotericin B against Fusarium oxysporum fungal strain with MIC of 0.98 µg/mL. Some of the test compounds showed remarkable cytotoxic activities against Hep G2 (hepatocellular carcinoma) cells (IC50=0.0158–71.3 µM) in comparison to the standard anticancer drug doxorubicin (IC50=0.008 µM). Among the compounds tested, (5), (6a), (6b), (7b), and (10) exhibited antiproliferative potency (IC50=0.0001–0.0211 µM) that was found to be better than that of doxorubicin (IC50=0.099 µM) against MCF7 (breast adenocarcinoma) cells. In particular, (7b) displayed the highest significant antiproliferative efficacy against both Hep G2 and MCF7 cell lines showing IC50 values of 0.0158 µM and 0.0001 µM, respectively. Our findings suggest that the synthesized compounds may be promising candidates as novel antimicrobial and antiproliferative agents.
収録刊行物
-
- Biological & Pharmaceutical Bulletin
-
Biological & Pharmaceutical Bulletin 39 (4), 473-483, 2016
公益社団法人 日本薬学会
- Tweet
キーワード
詳細情報 詳細情報について
-
- CRID
- 1390282679608489856
-
- NII論文ID
- 130005141687
-
- NII書誌ID
- AA10885497
-
- ISSN
- 13475215
- 09186158
-
- NDL書誌ID
- 027220609
-
- PubMed
- 27040621
-
- 本文言語コード
- en
-
- データソース種別
-
- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可