Synthesis and biological evaluation of polyaminated 2′,3′-dideoxy-3′-thiacytidine prodrugs

被引:2
|
作者
Camplo, M
Mourier, N
Chermann, JC
Kraus, JL
机构
[1] Univ Mediterrannee, Fac Sci Luminy, INSERM, U322,Lab Chim Biomol, F-13288 Marseille 9, France
[2] INSERM, Retrovirus & Maladies Assoc U322, F-13273 Marseille, France
来源
NUCLEOSIDES & NUCLEOTIDES | 1999年 / 18卷 / 4-5期
关键词
D O I
10.1080/15257779908041590
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
The syntheses and biological evaluation of polyaminated 2',3'-dideoxy-3'-thiacytidine have been performed. A new lead was found to increase the in vitro antiviral potency (syncitia formation on MT-4 cell line) of two order magnitude greater than the parent nucleoside drug. Moreover, the in vitro activity on HIV macrophages was found to be more than 3 log greater than the activity of the parent drug 1.
引用
收藏
页码:879 / 880
页数:2
相关论文
共 50 条
  • [1] Synthesis and anti-HIV evaluation of new 2′,3′-dideoxy-3′-thiacytidine prodrugs
    Mourier, N
    Camplo, M
    Della Bruna, GS
    Pellacini, F
    Ungheri, D
    Chermann, JC
    Kraus, JL
    NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS, 2000, 19 (07): : 1057 - 1091
  • [2] Synthesis and Biological Evaluation of Fatty Acyl Ester Derivatives of (-)-2′,3′-Dideoxy-3′-thiacytidine
    Agarwal, Hitesh K.
    Chhikara, Bhupender S.
    Hanley, Michael J.
    Ye, Guofeng
    Doncel, Gustavo F.
    Parang, Keykavous
    JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (10) : 4861 - 4871
  • [3] Synthesis and anti-HIV activity of novel 2′,3′-dideoxy-3′-thiacytidine prodrugs
    Ravetti, Soledad
    Gualdesi, Maria S.
    Trinchero-Hernandez, Juan S.
    Turk, Gabriela
    Brinon, Margarita C.
    BIOORGANIC & MEDICINAL CHEMISTRY, 2009, 17 (17) : 6407 - 6413
  • [4] BIOCHEMICAL PHARMACOLOGY OF (+)-2',3'-DIDEOXY-3'-THIACYTIDINE AND (-)-2',3'-DIDEOXY-3'-THIACYTIDINE AS ANTIHEPATITIS B-VIRUS AGENTS
    CHANG, CN
    SKALSKI, V
    ZHOU, JH
    CHENG, YC
    JOURNAL OF BIOLOGICAL CHEMISTRY, 1992, 267 (31) : 22414 - 22420
  • [5] Pharmacokinetics of (-)-2'-3'-dideoxy-3'-thiacytidine in woodchucks
    Rajagopalan, P
    Boudinot, FD
    Chu, CK
    Tennant, BC
    Baldwin, BH
    Schinazi, RF
    ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1996, 40 (03) : 642 - 645
  • [6] 5′-Phosphonate Derivatives of 2′,3′-Dideoxy-3′-Thiacytidine as New Anti-HIV Prodrugs
    Khandazhinskaya, Anastasia L.
    Jasko, Maxim V.
    Karpenko, Inna L.
    Solyev, Pavel N.
    Golubeva, Natalia A.
    Kukhanova, Marina K.
    CHEMICAL BIOLOGY & DRUG DESIGN, 2011, 78 (01) : 50 - 56
  • [7] SYNTHESIS AND ANTIVIRAL ACTIVITY OF NEW CARBONYLPHOSPHONATE 2',3'-DIDEOXY-3'-THIACYTIDINE CONJUGATES
    CHARVET, AS
    TURIN, F
    FAURY, P
    HANTZ, O
    CAMPLO, M
    MOURIER, N
    BERTHILLON, P
    GRACIET, JC
    CHERMANN, JC
    TREPO, C
    KRAUS, JL
    ANTIVIRAL RESEARCH, 1994, 25 (02) : 161 - 168
  • [8] Synthesis and biological evaluation of 2',3'-dideoxy-3'-fluororibofuranosyl purine nucleosides
    Poopeiko, NE
    Khripach, NB
    Kazimierczuk, Z
    Balzarini, J
    DeClercq, E
    Mikhailopulo, IA
    NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS, 1997, 16 (7-9): : 1083 - 1086
  • [9] Creation of a Long-Acting Nanoformulated 2′,3′-Dideoxy-3′-Thiacytidine
    Guo, Dongwei
    Zhou, Tian
    Arainga, Mariluz
    Palandri, Diana
    Gautam, Nagsen
    Bronich, Tatiana
    Alnouti, Yazen
    McMillan, JoEllyn
    Edagwa, Benson
    Gendelman, Howard E.
    JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES, 2017, 74 (03) : E75 - E83
  • [10] SYNTHESIS AND BIOLOGICAL EVALUATION OF A NEW N4-(N-FORMYL PEPTIDE)-2',3'-DIDEOXY-3'-THIACYTIDINE AS ANTI-HIV PRODRUG
    CAMPLO, M
    FAURY, P
    CHARVET, AS
    LEDERER, F
    CHERMANN, JC
    KRAUS, JL
    NUCLEOSIDES & NUCLEOTIDES, 1993, 12 (06): : 631 - 641