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Dive into the research topics where Shyi-Tai Jan is active.

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Featured researches published by Shyi-Tai Jan.


Bioorganic & Medicinal Chemistry Letters | 2000

Structure-based design of a novel synthetic spiroketal pyran as a pharmacophore for the marine natural product spongistatin 1

Fatih M. Uckun; Chen Mao; Alexei Vassilev; He Huang; Shyi-Tai Jan

SPIKET-P, a novel synthetic spiroketal pyran, was rationally designed as a pharmocophore for the tubulin depolymerizing marine natural product Spongistatin 1. SPIKET-P was prepared from the commercially available benzyl (R)-(-)-glycidyl ether using a versatile 11-step synthetic scheme in a stereocontrolled fashion. At nanomolar concentrations, SPIKET-P caused tubulin depolymerization in cell-free turbidity assays and exhibited potent cytotoxic activity against cancer cells as evidenced by destruction of microtubule organization, and prevention of mitotic spindle formation in human breast cancer cells.


British Journal of Haematology | 2010

Targeting SYK kinase-dependent anti-apoptotic resistance pathway in B-lineage acute lymphoblastic leukaemia (ALL) cells with a potent SYK inhibitory pentapeptide mimic.

Fatih M. Uckun; Rauf Onur Ek; Shyi-Tai Jan; Chun-Lin Chen; Sanjive Qazi

The present study found that the pentapeptide mimic C‐61, targeting the substrate binding P‐site of SYK tyrosine kinase acted as a potent inducer of apoptosis in chemotherapy‐resistant SYK‐expressing primary leukemic B‐cell precursors taken directly from relapsed B‐precursor leukaemia (BPL) patients (but not SYK‐deficient infant pro‐B leukaemia cells), exhibited favourable pharmacokinetics in mice and non‐human primates, and eradicated in vivo clonogenic leukaemia cells in severe combined immunodeficient mouse xenograft models of chemotherapy‐resistant human BPL at dose levels non‐toxic to mice and non‐human primates. These in vitro and in vivo findings provide proof of principle for effective treatment of chemotherapy‐resistant BPL by targeting SYK‐dependent anti‐apoptotic blast cell survival machinery with a SYK P‐Site inhibitor. Further development of C‐61 may provide the foundation for therapeutic innovation against chemotherapy‐resistant BPL.


Tetrahedron Letters | 2000

Stereocontrolled synthesis of a novel pharmacophore of the tubulin-depolymerizing marine natural product spongistatin

He Huang; Chen Mao; Shyi-Tai Jan; Fatih M. Uckun

Abstract We report here the synthesis and X-ray structure of a novel spiroketal pyran, SPIKET-P1, as a pharmocophore for the tubulin-depolymerizing marine natural product spongistatin 1. Following its retro-synthetic analysis, SPIKET-P1 was prepared using a versatile 11-step synthetic scheme in a stereocontrolled fashion.


Antiviral Chemistry & Chemotherapy | 1999

AZT-5′-(p-Bromophenyl Methoxyalaninyl Phosphate) as a Potent and Non-Toxic Anti-Human Immunodeficiency Virus Agent

Shyi-Tai Jan; Zhaohai Zhu; H-L Tai; Mei-Jue Shih; Taracad K. Venkatachalam; Fatih M. Uckun

The potency and selectivity index of the AZT-phenyl phosphate derivatives in thymidine kinase (TK)-deficient T cells were substantially enhanced by introducing a single para-bromo substituent in the phenyl moiety. AZT-5′-(p-bromophenyl methoxyalaninyl phosphate) was 43-fold more potent than AZT-5′-(phenyl methoxyalaninyl phosphate) and was fivefold more potent than AZT in inhibiting human immunodeficiency virus (HIV) replication in TK-deficient CEM cells.


Antiviral Chemistry & Chemotherapy | 1999

Synthesis of dual function (5R,6R)- and (5S,6S)-5-bromo-6-methoxy-5,6-dihydro-AZT-5'-(para-bromophenyl methoxyalaninyl phosphate) as novel spermicidal and anti-HIV agents.

Shyi-Tai Jan; Mei-Jue Shih; Taracad K. Venkatachalam; Osmond J. D'Cruz; Chun-Lin Chen; Fatih M. Uckun

We synthesized a novel compound, 5-bromo-6-methoxy-5,6-dihydro-AZT-5′-(p-bromophenyl methoxyalaninyl phosphate), which had an EC50 value of 5 µM in sperm motility assays. This is >1 log10 better than that of the detergent spermicide nonoxynol-9 (EC50 81 µM). The compound also displayed a potent anti-human immunodeficiency virus (HIV) activity with an IC50 value of 0.005 µM in HIV replication assays, which was virtually identical to that of AZT (IC50 0.006 µM) and >2 log10 more potent than that of nonoxynol-9 (IC50 2.2 µM). The promising results reported herein recommend the further development of the dual function 5-halo-6-alkoxyl-5,6-dihydro-AZT derivatives as a new class of vaginal contraceptives capable of preventing the sexual transmission of HIV while providing fertility control for women who are at high risk of acquiring HIV by heterosexual transmission. These dual function 5-halo-6-alkoxyl-5,6-dihydro-AZT derivatives may also have utility in curbing domestic and wildlife animal retroviral transmissions.


Tetrahedron Letters | 1999

Stereoselective synthesis of a versatile intermediate for the total synthesis of mono- and bis-THF containing annonaceous acetogenins

Shyi-Tai Jan; Keqiang Li; Shikha Vig; Alexander Rudolph; Fatih M. Uckun

Abstract Stereoselective synthesis of epoxy tetrahydrofuran (THF) 1 , a versatile synthetic precursor for mono-THF and bis-THF containing annonaceous acetogenins, is reported. Compound 1 was synthesized from tridecanal in 11 steps with an overall yield of 24%. The requisite configurations of the stereogenic centers in 1 were established by Sharpless asymmetric epoxidation and Sharpless asymmetric dihydroxylation. Formation of the THF-ring unit was accomplished by acid catalyzed epoxide ring opening and 5- exo cyclization reaction.


Bioorganic & Medicinal Chemistry Letters | 1998

Enhancing effects of a mono-bromo substitution at the para position of the phenyl moiety on the metabolism and anti-HIV activity of d4T-phenyl methoxyalaninyl phosphate derivatives.

Taracad K. Venkatachalam; Hung-Liang Tai; Rakesh Vig; Chun-Lin Chen; Shyi-Tai Jan; Fatih M. Uckun


Antiviral Chemistry & Chemotherapy | 1998

Aryl phosphate derivatives of 3'-deoxythymidine are not potent anti-human immunodeficiency virus agents.

Vig R; Venkatachalam Tk; Shyi-Tai Jan; Fatih M. Uckun


Archive | 2000

One pot synthesis of 5′-hydroxy phosphorylated nucleoside derivatives, and compounds formed thereby

Shyi-Tai Jan; Fatih M. Uckun


The Journal of Allergy and Clinical Immunology | 2000

1061 Tyrosine kinase inhibitor 2,4,6-trihydroxy-αp-methoxyphenylacetophenone (Compound D-58) Is a potent inhibitor of allergic and inflammatory reactions

Fatih M. Uckun; Rama Malaviya; Shyi-Tai Jan; De-Min Zhu; Ravi Malaviya

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Fatih M. Uckun

University of Southern California

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Alexander Rudolph

University of Texas at Austin

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Osmond J. D'Cruz

University of Oklahoma Health Sciences Center

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Rama Malaviya

Washington University in St. Louis

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Sanjive Qazi

Gustavus Adolphus College

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Rauf Onur Ek

Adnan Menderes University

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