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Showing articles posted using tag #Medicinal Chemistry (x)

Synthesis and Biological Evaluation of Fatty Acyl Ester Derivatives of (−)-2′,3′-Dideoxy-3′-thiacytidine
- Posted by Dr. Bhupender Singh
- May 29, 2012
- 0 comments
- 0 likes
- 402 views
A number of fatty acyl derivatives of (−)-2′,3′-dideoxy-3′-thiacytidine (lamivudine, 3TC, 1) were synthesized and evaluated for their anti-HIV activity. The monosubstituted 5′-O-fatty acyl derivatives of 3TC (EC50 = 0.2–2.3 μM) were more potent than th...
Synthesis and Anti-HIV Activities of Glutamate and Peptide Conjugates of Nucleoside Reverse Transcriptase Inhibitors
- Posted by Dr. Bhupender Singh
- April 11, 2012
- 0 comments
- 0 likes
- 460 views
Mono-, di-, and trinucleoside conjugates of glutamate or peptide scaffolds containing nucleoside reverse transcriptase inhibitors were synthesized. Among dinucleoside glutamate ester derivatives, N-myristoylated derivatives showed significantly hi...
Synthesis, Anticancer Activities, and Cellular Uptake Studies of Lipophilic Derivatives of Doxorubicin Succinate
- Posted by Dr. Bhupender Singh
- April 11, 2012
- 0 comments
- 0 likes
- 753 views
A number of lipophilic 14-substituted derivatives of doxorubicin were synthesized through conjugation of doxorubicin-14-hemisuccinate with different fatty amines or tetradecanol to enhance the lipophilicity, cellular uptake, and cellular retention for ...
CNT loading into cationic cholesterol suspensions show improved DNA binding and serum stability and ability to internalize into cancer cells
- Posted by Dr. Bhupender Singh
- February 24, 2012
- 1 comment
- 0 likes
- 336 views
Single walled carbon nanotubes were solubilized in water using synthesized Cholesterol lipids and conjugates evaluated for efficacy for oligonucleotide delivery in cancer cells.
One-pot regioselective synthesis of tetrahydroindazolones and evaluation of their anticancer and Src kinase inhibitory activities
- Posted by Dr. Bhupender Singh
- November 9, 2011
- 0 comments
- 0 likes
- 621 views
A number of 2-substituted tetrahydroindazolones were synthesized by three-component condensation reaction of 1,3-diketones, substituted hydrazines, benzaldehydes, and Yb(OTf)3 as a catalyst in [bmim][BF4] ionic liquid using a simple, efficient, an...
3-Substitued indoles: One-pot synthesis and evaluation of anticancer and Src kinase inhibitory activities
- Posted by Dr. Bhupender Singh
- August 15, 2011
- 0 comments
- 0 likes
- 645 views
An efficient and economical method was developed for the synthesis of 3-substituted indoles by one-pot three-component coupling reaction of a substituted or unsubstituted benzaldehyde, N-methylaniline, and indole or N-methylindole using Yb(OTf)3–...
Fatty-Acyl Amide Derivatives of Doxorubicin: Synthesis and In Vitro Anticancer Activities
- Posted by Dr. Bhupender Singh
- March 6, 2011
- 0 comments
- 1 like
- 1,772 views
Doxorubicin is an anti-neoplastic drug extensively used in anti-cancer therapy. It is highly hydrophilic with low biological life and have severe side effect with the applied overdoses. Moderation with the introduction of lipophilic group on doxorubici...
Synthesis of 3-Phenylpyrazolopyrimidine-1,2,3-Triazole Conjugates and Evaluation of their Src Kinase Inhibitory and Anticancer Activities
- Posted by Dr. Bhupender Singh
- now
- 0 comments
- 0 likes
- 1,338 views
A series of two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates were synthesized using click chemistry approach. All compounds were evaluated for inhibition of Src kinase and human ovarian adenocarcinoma (SK-Ov-3), breast carcinoma (MDA...
Development of cytarabine prodrugs and delivery systems for leukemia treatment
- Posted by Dr. Bhupender Singh
- now
- 0 comments
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- 969 views
Importance of the field: Cytarabine is a polar nucleoside drug used for the treatment of myeloid leukemia and non-Hodgkin's lymphoma. The drug has a short plasma half-life, low stability and limited bioavailability. Overdosing of patients with c...
Synthesis and evaluation of fatty acyl ester derivatives of cytarabine as anti-leukemia agents
- Posted by Dr. Bhupender Singh
- now
- 0 comments
- 0 likes
- 694 views
Cytarabine is a chemotherapeutic agent predominately used for the treatment of acute myeloid leukemia and lymphoblastic leukemia. Cytarabine is a polar nucleoside, has a short plasma half-life, and its use is associated with severe side effects. Fatty ...