biological screening;
chemical biology;
drug design;
APOPTOSIS;
DISCOVERY;
RESISTANT;
CANCER;
DRUGS;
CELLS;
D O I:
10.1111/cbdd.12164
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:
Cancer continues to be one of the biggest threats to the human civilization because there is no cure of it. Small heterocyclic molecule with low molecular weight and novel structural feature is therapeutically highly demanding. These molecules have the capability to disrupt signaling pathways leading to anticancer activities. Therefore, the search for new anticancer agents continues to draw attention to the research community. In this study, a small triazolo-benzoxazepine scaffolds was synthesized using a one-pot four-step synthetic methodology involving click reaction. Small libraries of 12 compounds were successfully synthesized and screened them against different cancer cell lines. Low micromolar anticancer activity was recorded using MTT assay, and further confirmation of cell death was obtained by phase contrast, fluorescent, and confocal images.
机构:
Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USAUniv Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA
Bhattacharyya, Roby P.
;
Remenyi, Attila
论文数: 0引用数: 0
h-index: 0
机构:
Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USAUniv Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA
Remenyi, Attila
;
Yeh, Brian J.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USAUniv Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA
Yeh, Brian J.
;
Lim, Wendell A.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USAUniv Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA
机构:
Cent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Chakravarti, Bandana
;
Siddiqui, Jawed A.
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Siddiqui, Jawed A.
;
Dwivedi, Shailendra K. Dhar
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Dwivedi, Shailendra K. Dhar
;
Deshpande, Shreekant
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Med & Proc Chem, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Deshpande, Shreekant
;
Samanta, Krishnanda
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Med & Proc Chem, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Samanta, Krishnanda
;
Bhatta, Rabi S.
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Pharmacokinet & Metab, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Bhatta, Rabi S.
;
Panda, Gautam
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Med & Proc Chem, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Panda, Gautam
;
Prabhakar, Yenamandra S.
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Med & Proc Chem, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Prabhakar, Yenamandra S.
;
Konwar, Rituraj
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Konwar, Rituraj
;
Sanyal, Sabaysachi
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Drug Target Discovery & Dev, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Sanyal, Sabaysachi
;
Chattopadhyay, Naibedya
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
机构:
Indian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Chandrasekhar, Srivari
;
Seenaiah, Mallikanti
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Seenaiah, Mallikanti
;
Kumar, Abhishek
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Kumar, Abhishek
;
Reddy, Chada Raji
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Reddy, Chada Raji
;
Mamidyala, Suman Kumar
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Biol Chem Lab, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Mamidyala, Suman Kumar
;
Kumar, Chityal Ganesh
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Biol Chem Lab, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Kumar, Chityal Ganesh
;
Balasubramanian, Sridhar
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Ctr Xray Crystallog, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
机构:
Karmanos Canc Inst, Dept Pharm, Detroit, MI USAWayne State Univ, Dept Internal Med, Karmanos Canc Inst, Detroit, MI 48202 USA
Cronin, Simon
;
Chandrasekar, Pranatharthi H.
论文数: 0引用数: 0
h-index: 0
机构:
Wayne State Univ, Dept Internal Med, Karmanos Canc Inst, Detroit, MI 48202 USAWayne State Univ, Dept Internal Med, Karmanos Canc Inst, Detroit, MI 48202 USA
机构:
Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USAUniv Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA
Bhattacharyya, Roby P.
;
Remenyi, Attila
论文数: 0引用数: 0
h-index: 0
机构:
Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USAUniv Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA
Remenyi, Attila
;
Yeh, Brian J.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USAUniv Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA
Yeh, Brian J.
;
Lim, Wendell A.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USAUniv Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA
机构:
Cent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Chakravarti, Bandana
;
Siddiqui, Jawed A.
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Siddiqui, Jawed A.
;
Dwivedi, Shailendra K. Dhar
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Dwivedi, Shailendra K. Dhar
;
Deshpande, Shreekant
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Med & Proc Chem, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Deshpande, Shreekant
;
Samanta, Krishnanda
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Med & Proc Chem, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Samanta, Krishnanda
;
Bhatta, Rabi S.
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Pharmacokinet & Metab, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Bhatta, Rabi S.
;
Panda, Gautam
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Med & Proc Chem, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Panda, Gautam
;
Prabhakar, Yenamandra S.
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Med & Proc Chem, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Prabhakar, Yenamandra S.
;
Konwar, Rituraj
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Konwar, Rituraj
;
Sanyal, Sabaysachi
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Drug Target Discovery & Dev, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
Sanyal, Sabaysachi
;
Chattopadhyay, Naibedya
论文数: 0引用数: 0
h-index: 0
机构:
Cent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, IndiaCent Drug Res Inst, Div Endocrinol, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India
机构:
Indian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Chandrasekhar, Srivari
;
Seenaiah, Mallikanti
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Seenaiah, Mallikanti
;
Kumar, Abhishek
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Kumar, Abhishek
;
Reddy, Chada Raji
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Reddy, Chada Raji
;
Mamidyala, Suman Kumar
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Biol Chem Lab, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Mamidyala, Suman Kumar
;
Kumar, Chityal Ganesh
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Biol Chem Lab, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
Kumar, Chityal Ganesh
;
Balasubramanian, Sridhar
论文数: 0引用数: 0
h-index: 0
机构:
Indian Inst Chem Technol, Ctr Xray Crystallog, Hyderabad 500007, Andhra Pradesh, IndiaIndian Inst Chem Technol, Organ Chem Div 1, Hyderabad 500007, Andhra Pradesh, India
机构:
Karmanos Canc Inst, Dept Pharm, Detroit, MI USAWayne State Univ, Dept Internal Med, Karmanos Canc Inst, Detroit, MI 48202 USA
Cronin, Simon
;
Chandrasekar, Pranatharthi H.
论文数: 0引用数: 0
h-index: 0
机构:
Wayne State Univ, Dept Internal Med, Karmanos Canc Inst, Detroit, MI 48202 USAWayne State Univ, Dept Internal Med, Karmanos Canc Inst, Detroit, MI 48202 USA