In th
is rev
iew, both cat
ion
ic and neutral synthet
ic l
igands that b
ind
in the m
inor groove of DNA are d
iscussed. Certa
in b
is-d
istamyc
ins and related lex
itrops
ins show act
iv
it
ies aga
inst human
immunodef
ic
iency v
irus (HIV)-1 and HIV-2 at low nanomolar concentrat
ions. DAPI b
inds strongly to AT-conta
in
ing polymers and
is located
in the m
inor groove of DNA. DAPI
intercalates
in DNA sequences that do not conta
in at least three consecut
ive AT bp. Beren
il can also exh
ib
it
intercalat
ive, as well as m
inor groove b
ind
ing, propert
ies depend
ing on sequence. Furan-conta
in
ing analogues of beren
il play an
important role
in the
ir act
iv
it
ies aga
inst <
i>Pneumocyst
is car
in
iii> and <
i>Cryptospor
id
ium parvuam
i>
infect
ions
in v
ivo. Pt(II)-beren
il conjugates show a good act
iv
ity prof
ile aga
inst HL60 and U-937 human leukem
ic cells. Pt-pentam
id
ine shows h
igher ant
iprol
iferat
ive act
iv
ity aga
inst small cell lung, non-small cell lung, and melanoma cancer cell l
ines compared w
ith many other tumor cell l
ines. <
i>trans
i>-Butenam
id
ine shows good ant
i-<
i>P. car
in
iii> act
iv
ity
in rats. Pentam
id
ine
is used aga
inst <
i>P. car
in
iii> pneumon
ia
in
ind
iv
iduals
infected w
ith HIV who are at h
igh r
isk from th
is
infect
ion. A compar
ison of the cytotox
ic potenc
ies of adozeles
in, b
izeles
in, carzeles
in, c
isplat
in, and doxorub
ic
in
ind
icates that adozeles
in
is a potent analog of CC-1065. Naturally occurr
ing pyrrolo[2,1-<
i>c
i>][1,4]benzod
iazep
ines such as anthramyc
in have a 2- to 3-bp sequence spec
if
ic
ity, but a synthet
ic PBD d
imer spans 6 bp, act
ively recogn
iz
ing a central 5&pr
ime;-GATC sequence. The crossl
ink
ing eff
ic
iency of PBD d
imers
is much greater than that of other major groove crossl
inkers, such as c
isplat
in, melphalan, etc. Neothramyc
in
is used cl
in
ically for the treatment of superf
ic
ial carc
inoma of the bladder.
idth=""100"" bgcolor=""#F0F0F0"" valign=""top""> ial"" size=""-1"" color=""black""> Publisher: | idth=""470"" valign=""top""> ial"" size=""-1"" color=""black""> Elsevier Science |
idth=""100"" bgcolor=""#F0F0F0"" valign=""top""> ial"" size=""-1"" color=""black""> Language of Publication: | idth=""470"" valign=""top""> ial"" size=""-1"" color=""black""> English |
idth=""100"" bgcolor=""#F0F0F0"" valign=""top""> ial"" size=""-1"" color=""black""> Item Identifier: | idth=""470"" valign=""top""> ial"" size=""-1"" color=""black""> S0163-7258(99)00021-2 |
idth=""100"" bgcolor=""#F0F0F0"" valign=""top""> ial"" size=""-1"" color=""black""> Publication Type: | idth=""470"" valign=""top""> ial"" size=""-1"" color=""black""> Article |
idth=""100"" bgcolor=""#F0F0F0"" valign=""top""> ial"" size=""-1"" color=""black""> ISSN: | idth=""470"" valign=""top""> ial"" size=""-1"" color=""black""> 0163-7258 |
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idth=""30""> | ize=""1""/>ial"" size=""-1"" color=""black""> Footnotes: i><i>Editor's Note:i> appear throughout text. Structures 1–271 appear together at the end of this article, although Structures 25, 111–147, 162–181, 182–188, and 241–255 also appear within .
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