Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells

被引：27

作者：

Al-Sanea, Mohammad M. ^{[1
]}

Al-Ansary, Ghada H. ^{[2
,3
]}

Elsayed, Zainab M. ^{[4
]}

Maklad, Raed M. ^{[5
,6
]}

Elkaeed, Eslam B. ^{[7
,8
]}

Abdelgawad, Mohamed A. ^{[1
,9
]}

Bukhari, Syed Nasir Abbas ^{[1
]}

Abdel-Aziz, Marwa M. ^{[10
]}

Suliman, Howayda ^{[11
]}

Eldehna, Wagdy M. ^{[5
]}

机构：

[1] Jouf Univ, Coll Pharm, Dept Pharmaceut Chem, Sakaka 72341, Saudi Arabia

[2] Batterejee Med Coll, Dept Pharmaceut Chem, Pharm Program, Jeddah, Saudi Arabia

[3] Ain Shams Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, Egypt

[4] Kafrelsheikh Univ, Fac Pharm, Sci Res & Innovat Support Unit, Kafrelsheikh, Egypt

[5] Kafrelsheikh Univ, Fac Pharm, Dept Pharmaceut Chem, Kafrelsheikh 33516, Egypt

[6] Kafrelsheikh Univ, Inst Drug Discovery & Dev, Kafrelsheikh, Egypt

[7] AlMaarefa Univ, Coll Pharm, Dept Pharmaceut Sci, Riyadh, Saudi Arabia

[8] Al Azhar Univ, Fac Pharm Boys, Dept Pharmaceut Organ Chem, Cairo, Egypt

[9] Beni Suef Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Bani Suwayf, Egypt

[10] Al Azhar Univ, Reg Ctr Mycol & Biotechnol, Cairo, Egypt

[11] Alexandria Univ, Fac Med, Dept Med Biochem, Alexandria, Egypt

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2021年 / 36卷 / 01期

关键词：

Benzofuran-2-carbohydrazide; anticancer agents; lung cancer; VEGFR-2; inhibitors; BENZOFURAN DERIVATIVES; BIOLOGICAL EVALUATION; INHIBITORS SYNTHESIS; ANTICANCER ACTIVITY; DESIGN; FRUQUINTINIB; HYBRIDS; GROWTH; POTENT;

D O I：

10.1080/14756366.2021.1915302

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

As one of the most lethal malignancies, lung cancer is considered to account for approximately one-fifth of all malignant tumours-related deaths worldwide. This study reports the synthesis and in vitro biological assessment of two sets of 3-methylbenzofurans (4a-d, 6a-c, 8a-c and 11) and 3-(morpholinomethyl)benzofurans (15a-c, 16a-b, 17a-b and 18) as potential anticancer agents towards non-small cell lung carcinoma A549 and NCI-H23 cell lines, with VEGFR-2 inhibitory activity. The target benzofuran-based derivatives efficiently inhibited the growth of both A549 and NCI-H23 cell lines with IC50 spanning in ranges 1.48-47.02 and 0.49-68.9 mu M, respectively. The three most active benzofurans (4b, 15a and 16a) were further investigated for their effects on the cell cycle progression and apoptosis in A549 (for 4b) and NCI-H23 (for 15a and 16a) cell lines. Furthermore, benzofurans 4b, 15a and 16a displayed good VEGFR-2 inhibitory activity with IC50 equal 77.97, 132.5 and 45.4 nM, respectively.

引用

页码：987 / 999

页数：13

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