• Archives of Pharmacal Research
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• v.17 no.6
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• pp.467-469
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• 1994

Some Mannich bases of Antineoplaston A10 which is antitumor agent under chlinical investigation were synthesized and tested fro cytotoxicity. The tested compounds (2a, 2b, 2d) showed good activity comparable to that of carboplatin.

• Korean Journal of Plant Resources
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• v.5 no.2
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• pp.73-84
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• 1992

Many types of compounds have been isolated from higher plants till now, that is, alkaloids, terpenes, lignans, steroids and so on. One of them, named as RA series Cyclic hexapeptides isolated from Rubia akane and R. cordijofia also have strong antineoplastic activity against various types of tumors. Till now 10 kinds ofRA series compounds were isolated and named as RA - I, II, III, IV, V, VI, VII, VIII, IX and X. Moreover,monogl-ucoside of RA - V newly Isolated from same plant. Many kinds of derivatives including natural RAcompounds were tested for QSAR, and one of them, RA - VII was screened up as a most suitable substance asan antitumor agent. RA - VII(=RA-700) has strong cytotoxic activity against KB cells, P388 Iymphocyticleukemia and MM2 mammary carcinoma cells. RA - VII has been under investigation for Phase I clinical trials.

• Archives of Pharmacal Research
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• v.22 no.6
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• pp.575-578
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• 1999

Derivatives of elema-1,3-diene were synthesized in several steps as polar analogs of $\beta$-elemene, antitumor agent under clinical phase. The lactone ring of compound 1 was opened by LiAlH4 to give diol 2 which was selectively protected by TBDPSCI. After acetylation of the secondary alcohol, the acetylated product was ozonolyzed and reduced to give elemene derivative 4 which was converted to diolefin 8 via selenides subsequent deprotection by tetrabutylammonium fluoride gave two compounds 9, 10.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.233.3-234
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• 2002

SB31, an extract of Pulsatilla koreana, has been tried as an antitumor agent by traditional medicine pratitioner in Korea for the past 30 years, SB31 was evaluated for cytotoxic and antitumor activity against a variety of cancer cell lines. The SB31 exhibited 5-6 fold less cytotoxic activity against normal mononuclear cells (ED$\sub$50/. 1.1 mg/$m\ell$) than against cancer cell lines (ED$\sub$50/ 0.14-0.19mg/$m\ell$). (omitted)

• KSBB Journal
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• v.13 no.6
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• pp.669-674
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• 1998

This study was carried out particularly focusing on he antitumor effect in combination with 5-fluorocytosine(5-FC), antifungal agent, and extracellular cytosine deaminase from Chromobacterium violaceum YK 391 against U-937, K-562 and SNU-C4 cells. While the addition of 10$\mu\textrm{g}$/100 ${\mu}\ell$ of anticancer agent, 5-fluorouracil(5-FU), to U-937, K-562 and SNU-C4 caused the decrease of proliferation 90%, 75% and 93% respectively, the addition of 20 $\mu\textrm{g}$/100 ${\mu}\ell$ of the extracellular cytosine deaminase and 10 $\mu\textrm{g}$/100 ${\mu}\ell$ of antifungal agent 5-FC caused the decrease of proliferation 80%, 70% and 90%, respectively. These results, therefore, reveal that this enzyme has the similar clinical effect for considering of adjuvant antitumor effect. From the above results, the treatment of 5-FC and the cytosine deaminase was very effective and showed the possibility to remove side effects which easily occur by the treatment of 5-FU only. An extracellular cytosine deaminase.

• KSBB Journal
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• v.17 no.6
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• pp.520-524
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• 2002

The present study was designed to investigate the effects of Stachys Sieboldii MIQ as a new natural antitumor agent or immunomodulator. To obtain the above objectives, Stachys sieboldii MIQ was extracted with ethanol. Stachys sieboldii MIQ accelerated mouse spleen cell growth, but inhibited FM3A/S°-cell growth. However, no significant difference was found for CD4+ / CD8+ cells. The growth rates of CD4+ and CD8+ T cells were accelerated more than those normal mouse group. Stachys sieboldii MIQ fed mice showed a significant enhancement of IL-2 receptor expression, increased numbers of CD4+ T cells, and CD8+ T cells. Stachys sieboldii MIQ also stimulated the production of NO by peritoneal macrophages and the production of NO by and the growth of mouse spleen cells. On the other hand, lung localization of Bl6Fl0 melanoma cells was inhibited by ethanol extract of Stachys sieboldii MIQ. These results show that Stachys sieboldii MIQ is a useful new functional antitumor agent or immunomodulator.

• Archives of Pharmacal Research
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• v.21 no.2
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• pp.157-163
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• 1998

Several aniline mustard analogues were obtained by introducing N,N-bis(2-chloroethyl)amino moiety to phenyl ring of A10 analogues in order to increase reactivity of A10 analogs and selectivity into DNA. The in vitro antitumor activity of synthesized compounds was evaluated using five different solid tumor cell lines by SRB method. Aniline mustard analogues exhibited more potent antitumor activity than A10 analogs. Especially, m-aniline mustard of benzoyl analogue displayed remarkable antitumor activity.

• YAKHAK HOEJI
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• v.47 no.6
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• pp.345-351
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• 2003

Heptaplatin, cis-Malonato[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II), is a novel platinum-based antitumor agent with clinical potential against human stomach cancer and the 3rd generation of the cisplatin. This study was performed to study how cisplain, heptaplatin and sunpla which is a mixture of heptaplatin and mannitol (w: w=l : 2) affect cell viability of SK-MEL-28 human melanoma cell line. Heptaplatin ($IC_{50}$/; 95.35 $\mu$M) and sunpla ($IC_{50}$/; 10.95 11M) were less effect than cisplatin (IC $_{50}$; 10.92 $\mu$M) on the SK-MEL-28 cells. By cell cycle analysis using flow cytometry, it was identified that the cells were arrested at G2/M phase by cisplatin, heptaplatin and sunpla, and percentage of cell death group was increased according to increasing of time and concentration. These results suggest that cisplatin, heptaplatin and sunpla are a novel anticancer agent against human melanoma cell.l.

• Archives of Pharmacal Research
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• v.20 no.2
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• pp.138-143
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• 1997

5-Aryl-2,3-dihydroimidazo[2,1-a]isoquinolines were reported to have strong antitumor activity and one of the derivatives such as $5-[4^{l}$ -(piperidinomethyl)phenyl]-2,3-dihydroimidazo[2,1-a] isoquinoline (1, SDZ 62-434) was found to be more effective than the clinical cytostatic agent edelfosine (2) in in vitro and in vivo assays. Currently SDZ 62-434 is in clinical trials in Europe. The structure-activity relationship studies of SDZ 62-434 showed that compounds with substitution on ring A were less active than the lead compound. Ring B in SDZ 62-434 was essential for the activity because compounds without B ring had no antitumor activity. Among the 3-arylisoquinolin-1-one derivatives, $3-[4^{I}$-(piperidinomethyl)phenyl] substituted analog had no antitumor activity but simple phenyl substituted compound, such as 4, showed the most potent antitumor activity in various human tumor cell lines.

• Archives of Pharmacal Research
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• v.21 no.2
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• pp.193-197
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• 1998

A number of substituted isoquinolin-1-ones, possible bioisosteres of the 5-aryl substituted 2,3-dihydroimidazo[2,$1-a$]isoquinolines, were synthesized and tested for their antitumor activity against five different human tumor cell lines. O-(3-hydroxyporpyl) substituted compound (15) exhibited the best antitumor activity which is 3-5 times better than 5-[$4^1$-(piperidinomethyl)phenyl]-2,3-dihydroimidazo[2,$1-a$]isoquinoline (1).